HRP20221030T1 - Heterociklički spojevi kao imunomodulatori - Google Patents

Heterociklički spojevi kao imunomodulatori Download PDF

Info

Publication number
HRP20221030T1
HRP20221030T1 HRP20221030TT HRP20221030T HRP20221030T1 HR P20221030 T1 HRP20221030 T1 HR P20221030T1 HR P20221030T T HRP20221030T T HR P20221030TT HR P20221030 T HRP20221030 T HR P20221030T HR P20221030 T1 HRP20221030 T1 HR P20221030T1
Authority
HR
Croatia
Prior art keywords
alkyl
cycloalkyl
haloalkyl
aryl
independently selected
Prior art date
Application number
HRP20221030TT
Other languages
English (en)
Inventor
Kaijiong Xiao
Fenglei Zhang
Liangxing Wu
Wenqing Yao
Original Assignee
Incyte Corporation
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Incyte Corporation filed Critical Incyte Corporation
Publication of HRP20221030T1 publication Critical patent/HRP20221030T1/hr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D515/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Claims (18)

1. Spoj s formulom (I): [image] ili njegova farmaceutski prihvatljiva sol ili stereoizomer, pri čemu: (i) G1 je NR6 i G2 je CR7R7; ili (ii) G1 je CR6R6 i G2 je NR7; skupina: [image] je odabrana od: [image] [image] i [image] X1 je N ili CR1; X2 je N ili CR2; X3 je N ili CR3; Cy je fenil, 2-tiofenil, 3-tiofenil, 2-piridil, 3-piridil, 4-piridil, 3,6-dihidro-2H-piran-4-il, cikloheksil, cikloheksenil, 2,3-dihidro-1,4-benzodioksin-6-il, 1,3-benzodioksin-5-il, 2-metilindazol-6-il ili 1-metilindazol-4-il, od kojih je svaki po izboru supstituiran s 1 do 5 neovisno odabranih supstituenata R8; R1, R2 i R3 su svaki neovisno odabrani iz niza koji sadrži H, C1-4 alkil, C3-10 cikloalkil, C3-10 cikloalkil-C1-4 alkil-, C6-10 aril, C6-10 aril-C1-4 alkil-, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, (5-10 člani heteroaril)-C1-4 alkil-, (4-10 člani heterocikloalkil)-C1-4 alkil-, C2-4 alkenil, C2-4 alkinil, halo, CN, OR10, C1-4 haloalkil, C1-4 haloalkoksi, NH2, -NHR10, -NR10R10, NHOR10, C(O)R10, C(O)NR10R10, C(O)OR10, OC(O)R10, OC(O)NR10R10, NR10C(O)R10, NR10C(O)OR10, NR10C(O)NR10R10, C(=NR10)R10, C(=NR10)NR10R10, NR10C(=NR10)NR10R10, NR10S(O)R10, NR10S(O)2R10, NR10S(O)2NR10R10, S(O)R10, S(O)NR10R10, S(O)2R10, i S(O)2NR10R10, pri čemu svaki R10 je neovisno odabran iz niza koji sadrži H, C1-4 alkil, C2-4 alkenil, C2-4 alkinil, C1-4 alkoksi, C3-10 cikloalkil, C3-10 cikloalkil-C1-4 alkil-, C6-10 aril, C6-10 aril-C1-4 alkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil-, pri čemu C1-4 alkil, C2-4 alkenil, C2-4 alkinil, C1-4 alkoksi, C3-10 cikloalkil, C3-10 cikloalkil-C1-4 alkil-, C6-10 aril, C6-10 aril-C1-4 alkil-, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil- od R1, R2, R3 i R10 su svaki po izboru supstituirani s 1, 2 ili 3 neovisno odabrana supstituenta Rd; R4, R5, R6, R7 i R8 su svaki neovisno odabrani iz niza koji sadrži H, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C1-6 haloalkoksi, C6-10 aril, C3-10 cikloalkil, 5-14 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-14 člani heteroaril)-C1-4 alkil-, (4-10 člani heterocikloalkil)-Ci-4 alkil-, CN, NO2, ORa, SRa, NHORa, C(O)Ra, C(O)NRaRa, C(O)ORa, OC(O)Ra, OC(O)NRaRa, NHRa, NRaRa, NRaC(O)Ra, NRaC(O)ORa, NRaC(O)NRaRa, C(=NRa)Ra, C(=NRa)NRaRa, NRaC(=NRa)NRaRa, NRaC(=NOH)NRaRa, NRaC(=NCN)NRaRa, NRaS(O)Ra, NRaS(O)2Ra, NRaS(O)2NRaRa, S(O)Ra, S(O)NRaRa, S(O)2Ra, i S(O)2NRaRa, pri čemu C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-14 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil- , C3-10 cikloalkil-C1-4 alkil-, (5-14 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil- od R4, R5, R6, R7 i R8 su svaki po izboru supstituirani s 1, 2, 3, 4 ili 5 supstituenata Rb; ili dva susjedna R8 supstituenta na Cy prstenu, uzeti zajedno s atomima na koje su oni vezani, tvore kondenzirani fenilni prsten, kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten, kondenzirani 5- ili 6-člani heteroarilni prsten ili kondenzirani C3-6 cikloalkilni prsten, pri čemu kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten i kondenzirani 5- ili 6-člani heteroarilni prsten svaki imaju 1-4 heteroatoma kao članove prstena odabrane između N, O i S i pri čemu kondenzirani fenilni prsten, kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten, kondenzirani 5- ili 6-člani heteroarilni prsten i kondenzirani C3-6 cikloalkilni prsten su svaki po izboru supstituirani s 1, 2 ili 3 neovisno odabrana supstituenta Rb; ili dva R5 supstituenta vezana na isti ugljikov atom, uzeti zajedno s ugljikovim atomom na koji su oni vezani, tvore C3-6 cikloalkilni prsten ili 4-, 5-, 6- ili 7-člani heterocikloalkilni prsten, pri čemu su C3-6 cikloalkilni prsten i 4-, 5-, 6- ili 7-člani heterocikloalkilni prsten svaki po izboru supstituirani s 1, 2 ili 3 neovisno odabrana supstituenta Rb; R9 je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C1-6 haloalkoksi, C6-10 aril, C3-10 cikloalkil, 5-14 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-14 člani heteroaril)-C1-4 alkil-, (4-10 člani heterocikloalkil)-C1-4 alkil-, CN, NO2, OR11, SR11, NH2, NHR11, NR11R11, NHOR11, C(O)R11, C(O)NR11R11, C(O)OR11, OC(O)R11, OC(O)NR11R11, NR11C(O)R11, NR11C(O)OR11, NR11C(O)NR11R11, C(=NR11)R11, C(=NR11)NR11R11, NR11C(=NR11)NR11R11, NR11C(=NOH)NR11R11, NR11C(=NCN)NR11R11, NR11S(O)R11, NR11S(O)2R11, NR11S(O)2NR11R11, S(O)R11, S(O)NR11R11, S(O)2R11, ili S(O)2NR11R11, pri čemu C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C1-6 haloalkoksi, C6-10 aril, C3-10 cikloalkil, 5-14 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-14 člani heteroaril)-C1-4 alkil- i (4-10 člani heterocikloalkil)-C1-4 alkil- od R9 su svaki po izboru supstituirani s 1, 2 ili 3 supstituenta Rb; svaki R11 je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil-, pri čemu C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil- i (4-10 člani heterocikloalkil)-C1-4 alkil- od R11 su svaki po izboru supstituirani s 1, 2 ili 3 supstituenta Rb; svaki Ra je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil-, pri čemu C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil- i (4-10 člani heterocikloalkil)-C1-4 alkil- od Ra su svaki po izboru supstituirani s 1, 2 ili 3 supstituenta Rd; svaki Rb supstituent je neovisno odabran iz niza koji sadrži halo, C1-6 alkil, C1-6 haloalkil, C1-6 haloalkoksi, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, (4-10 člani heterocikloalkil)-C1-4 alkil-, CN, OH, NH2, NO2, NHORc, ORc, SRc, C(O)Rc, C(O)NRcRc, C(O)ORc, OC(O)Rc, OC(O)NRcRc, C(=NRc)NRcRc, NRcC(=NRc)NRcRc, NRcC(=NOH)NRcRc, NRcC(=NCN)NRcW, NHRc, NRcRc, NRcC(O)Rc, NRcC(O)ORc, NRcC(O)NRCRc, NRcS(O)Rc, NRcS(O)2Rc, NRcS(O)2NRcRC, S(O)Rc, S(O)NRcRc, S(O)2Rc i S(O)2NRcRc; pri čemu C1-6 alkil, C1-6 haloalkil, C1-6 haloalkoksi, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-i (4-10 člani heterocikloalkil)-C1-4 alkil- od RB su svaki dalje po izboru supstituirani s 1-3 neovisno odabrana supstituenta Rd; svaki Rc je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil-, pri čemu C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil- i (4-10 člani heterocikloalkil)-C1-4 alkil- od Rc su svaki po izboru supstituirani s 1, 2 ili 3 supstituenta Rf neovisno odabrana iz niza koji sadrži C1-6 alkil, C1-6 haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, (4-10 člani heterocikloalkil)-C1-4 alkil-, halo, CN, NHORg, ORg, SRg, C(O)Rg, C(O)NRgRg, C(O)ORg, OC(O)Rg, OC(O)NRgRg, NHRg, NRgRg, NRgC(O)Rg, NRgC(O)NRgRg, NRgC(O)ORg, C(=NRg)NRgRg, NRgC(=NRg)NRgRg, NRgC(=NOH)NRgRg, NRgC(=NCN)NRgRg, S(O)Rg, S(O)NRgRg, S(O)2Rg, NRgS(O)2Rg, NRgS(O)2NRgRg, i S(O)2NRgRg; pri čemu C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil- od Rf su svaki po izboru supstituirani s 1, 2 ili 3 supstituenta Rn neovisno odabrana iz niza koji sadrži C1-6 alkil, C1-6 haloalkil, halo, CN, fenil, C3-6 cikloalkil, 5-6 člani heteroaril, 4-6 člani heterocikloalkil, NHOR°, OR°, SR°, C(O)R°, C(O)NR°R°, C(O)OR°, OC(O)R°, OC(O)NR°R°, NHR°, NR°R°, NR°C(O)R°, NR°C(O)NR°R°, NR°C(O)OR°, C(=NR°)NR°R°, NR°C(=NR°)NR°R°, S(O)R°, S(O)NR°R°, S(O)2R°, NR°S(O)2R°, NR°S(O)2NR°R°, i S(O)2NR°R°, pri čemu C1-6 alkil, C1-6 haloalkil, fenil, C3-6 cikloalkil, 5-6 člani heteroaril, i 4-6 člani heterocikloalkil od Rn je po izboru supstituiran s 1, 2 ili 3 supstituenta Rq; svaki Rd je neovisno odabran iz niza koji sadrži C1-6 alkil, C1-6 haloalkil, halo, C6-10 aril, 5-10 člani heteroaril, C3-10 cikloalkil, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil- , C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, (4-10 člani heterocikloalkil)-C1-4 alkil-, CN, NH2, NHORe, ORe, SRe, C(O)Re, C(O)NReRe, C(O)ORe, OC(O)Re, OC(O)NReRe, NHRe, NReRe, NReC(O)Re, NReC(O)NReRe, NReC(O)ORe, C(=NRe)NReRe, NReC(=NRe)NReRe, NReC(=NOH)NReRe, NReC(=NCN)NReRe, S(O)Re, S(O)NReRe, S(O)2R, NReS(O)2Re, NReS(O)2NReRe, i S(O)2NReRe, pri čemu C1-6 alkil, C1-6 haloalkil, C6-10 aril, 5-10 člani heteroaril, C3-10 cikloalkil, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil- od Rd su svaki po izboru supstituirani s 1-3 neovisno odabrana supstituenta Rf; svaki Re je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil-, pri čemu C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil- i (4-10 člani heterocikloalkil)-C1-4 alkil- od Re su svaki po izboru supstituirani s 1, 2 ili 3 neovisno odabrana supstituenta Rf; svaki Rg je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil-, pri čemu C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil- i (4-10 člani heterocikloalkil)-C1-4 alkil- od Rg su svaki po izboru supstituirani s 1-3 supstituenta Rp neovisno odabrana iz niza koji sadrži C1-6 alkil, C1-6haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, (4-10 člani heterocikloalkil)-C1-4 alkil-, halo, CN, NHORr, ORr, SRr, C(O)Rr, C(O)NRrRr, C(O)ORr, OC(O)Rr, OC(O)NRrRr, NHRr, NRrRr, NRrC(O)Rr, NRrC(O)NRrR.r, NRrC(O)ORr, C(=NRr)NRrRr, NRrC(=NRr)NRrRr, NRrC(=NOH)NRrRr, NRrC(=NCN)NRrRr, S(O)Rr, S(O)NRrRr, S(O)2Rr, NRrS(O)2Rr, NRrS(O)2NRrRr i S(O)2NRrRr, pri čemu C1-6 alkil, C1-6 haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil- i (4-10 člani heterocikloalkil)-C1-4 alkil- od Rp su svaki po izboru supstituirani s 1, 2 ili 3 supstituenta Rq; ili bilo koja dva supstituenta Ra zajedno s dušikovim atomom na koji su oni vezani tvore 4-, 5-, 6-, 7-, 8-, 9- ili 10-članu heterocikloalkilnu skupinu po izboru supstituiranu s 1, 2 ili 3 supstituenta Rh neovisno odabrana iz niza koji sadrži C1-6 alkil, C1-6 haloalkil, C3-10 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, 5-6 člani heteroaril, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-6 člani heteroaril)-C1-4 alkil-, (4-7 člani heterocikloalkil)-C1-4 alkil-, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, halo, CN, ORi, SRi, NHORi, C(O)Ri, C(O)NRiRi, C(O)ORi, OC(O)Ri, OC(O)NRiRi, NHRi, NRiRi, NRiC(O)Ri, NRiC(O)NRiRi, NRiC(O)ORi, C(=NRi)NRiRi, NRiC(=NRi)NRiRi, NRiC(=NOH)NRiRi, NRiC(=NCN)NRiRi, S(O)Ri, S(O)NRiRi, S(O)2Ri, NRiS(O)2Ri, NRiS(O)2NRiRi, i S(O)2NRiRi, pri čemu C1-6 alkil, C1-6 haloalkil, C3-10 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, 5-6 člani heteroaril, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-6 člani heteroaril)-C1-4 alkil-, (4-7 člani heterocikloalkil)-C1-4 alkil- od Rh su svaki izborno supstituirani s 1, 2, ili 3 supstituenta Rj neovisno odabrana iz niza koji sadrži C1-4 alkil, C3-6 cikloalkil, C6-10 aril, 5- ili 6-člani heteroaril, 4-6 člani heterocikloalkil, C2-4 alkenil, C2-4 alkinil, halo, C1-4 haloalkil, Ci-4haloalkoksi, CN, NHORk, ORk, SRk, C(O)Rk, C(O)NRkRk, C(O)ORk, OC(O)Rk, OC(O)NRkRk, NHRk, NRkRk, NRkC(O)Rk, NRkC(O)NRkRk, NRkC(O)ORk, C(=NRk)NRkRk, NRkC(=NRk)NRkRk, S(O)Rk, S(O)NRkRk, S(O)2Rk, NRkS(O)2Rk, NRkS(O)2NRkRk, i S(O)2NRkRk, pri čemu C1-4 alkil, C3-6 cikloalkil, C6-10 aril, 5- ili 6-člani heteroaril, 4-6 člani heterocikloalkil, C2-4 alkenil, C2-4 alkinil, C1-4 haloalkil, i C1-4haloalkoksi od Rj su svaki po izboru supstituirani s 1, 2 ili 3 supstituenta Rq; ili dvije Rh skupine vezane na isti atom ugljika 4- do 10-eročlanog heterocikloalkila, uzete zajedno s atomom ugljika na koji su vezane, tvore C3-6 cikloalkil ili 4- do 6-člani heterocikloalkil koji ima 1-2 heteroatoma kao članove prstena odabrane između O, N i S; svaki Ri ili Rk je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil-, pri čemu C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil- , (5-10 člani heteroaril)-C1-4 alkil- i (4-10 člani heterocikloalkil)-C1-4 alkil- od Ri ili Rk su svaki po izboru supstituirani s 1-3 neovisno odabrana supstituenta Rp; ili bilo koja dva supstituenta Rc zajedno s dušikovim atomom na koji su oni vezani tvore 4-, 5-, 6-, ili 7-članu heterocikloalkilnu skupinu po izboru supstituiranu s 1, 2, ili 3 neovisno odabrana supstituenta Rh; ili bilo koja dva supstituenta Re zajedno s dušikovim atomom na koji su oni vezani tvore 4-, 5-, 6-, ili 7-članu heterocikloalkilnu skupinu po izboru supstituiranu s 1, 2, ili 3 neovisno odabrana supstituenta Rh; ili bilo koja dva supstituenta Rg zajedno s dušikovim atomom na koji su oni vezani tvore 4-, 5-, 6-, ili 7-članu heterocikloalkilnu skupinu po izboru supstituiranu s 1, 2, ili 3 neovisno odabrana supstituenta Rh; ili bilo koja dva supstituenta Ro zajedno s dušikovim atomom na koji su oni vezani tvore 4-, 5-, 6-, ili 7-članu heterocikloalkilnu skupinu po izboru supstituiranu s 1, 2, ili 3 neovisno odabrana supstituenta Rh; ili bilo koja dva supstituenta Rr zajedno s dušikovim atomom na koji su oni vezani tvore 4-, 5-, 6-, ili 7-članu heterocikloalkilnu skupinu po izboru supstituiranu s 1, 2, ili 3 neovisno odabrana supstituenta Rh; svaki Ro ili Rr je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C3-6 cikloalkil, C6-10 aril, 4-6 člani heterocikloalkil, 5 ili 6-člani heteroaril, C1-4 haloalkil, C2-4 alkenil, i C2-4 alkinil, pri čemu C1-4 alkil, C1-6 haloalkil, C3-6 cikloalkil, C6-10 aril, 4-6 člani heterocikloalkil, 5 ili 6-člani heteroaril, C2-4 alkenil, i C2-4 alkinil od Ro ili Rr su svaki po izboru supstituirani s 1, 2 ili 3 supstituenta Rq; svaki Rq je neovisno odabran iz niza koji sadrži OH, CN, -COOH, NH2, halo, C1-6 haloalkil, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkoksi, C1-6 alkiltio, fenil, 5-6 člani heteroaril, 4-6 člani heterocikloalkil, C3-6 cikloalkil, NHR12 i NR12R12, pri čemu C1-6 alkil, fenil, C3-6 cikloalkil, 4-6 člani heterocikloalkil, i 5-6 člani heteroaril od Rq su svaki po izboru supstituirani s halo, OH, CN, -COOH, NH2, C1-4 alkoksi, C1-4 haloalkil, C1-4 haloalkoksi, fenil, C3-10 cikloalkil, 5-6 člani heteroaril i 4-6 člani heterocikloalkil i svaki R12 je neovisno C1-6 alkil; [image] je jednostruka veza ili dvostruka veza kako bi prsten A bio aromatski; i indeks n je cijeli broj 1, 2, 3 ili 4.
2. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol ili stereoizomer, naznačen time što: R1, R2 i R3 su svaki neovisno odabrani iz niza koji sadrži H, C1-4 alkil, C3-6 cikloalkil, C2-4 alkenil, C2-4 alkinil, halo, CN, OH, C1-4 alkoksi, C1-4 haloalkil, C1-4 haloalkoksi, NH2, -NH-C1-4 alkil, -N(C1-4 alkil)2, NHOR10, C(O)R10, C(O)NR10R10, C(O)OR10, OC(O)R10, OC(O)NR10R10, NR10C(O)R10, NR10C(O)OR10, NR10C(O)NR10R10, C(=NR10)R10, C(=NR10)NR10R10, NR10C(=NR10)NR10R10, NR10S(O)R10, NR10S(O)2R10, NR10S(0)2NR10R10, S(O)R10, S(O)NR10R10, S(O)2R10, i S(O)2NR pri čemu svaki R10 je neovisno odabran iz niza koji sadrži H i C1-4 alkil po izboru supstituiran s 1 ili 2 skupine neovisno odabrane od halo, OH, CN i C1-4 alkoksi; i pri čemu C1-4 alkil, C3-6 cikloalkil, C2-4 alkenil, C2-4 alkinil i C1-4 alkoksi od R1, R2 i R3 su svaki po izboru supstituirani s 1 ili 2 supstituenta neovisno odabrana iz niza koji sadrži halo, OH, CN i C1-4 alkoksi.
3. Spoj prema zahtjevu 1, naznačen time što ima: a) Formulu (II): [image] ili njegova farmaceutski prihvatljiva sol ili stereoizomer; ili b) Formulu (III): [image] ili njegova farmaceutski prihvatljiva sol ili stereoizomer; ili c) Formulu (IV): [image] ili njegova farmaceutski prihvatljiva sol ili stereoizomer; ili d) Formulu (V): [image] ili njegova farmaceutski prihvatljiva sol ili stereoizomer; ili e) Formulu (VI): [image] ili njegova farmaceutski prihvatljiva sol ili stereoizomer; ili f) Formulu (VII): [image] ili njegova farmaceutski prihvatljiva sol ili stereoizomer.
4. Spoj prema bilo kojem od zahtjeva 1-3, ili njegova farmaceutski prihvatljiva sol ili stereoizomer, naznačen time što: a) R1, R2 i R3 su svaki neovisno odabrani iz niza koji sadrži H, C1-4 alkil, C2-4 alkenil, C2-4 alkinil, halo, CN, OH, C1-4 alkoksi, C1-4 haloalkil, i C1-4 haloalkoksi; ili b) R1 je H, R2 je H ili halo, i R3 je H.
5. Spoj prema bilo kojem od zahtjeva 1-4, ili njegova farmaceutski prihvatljiva sol ili stereoizomer, naznačen time što: a) R9 je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C1-6 haloalkoksi, CN, NO2, ili NH2; ili b) R9 je halo, C1-6 alkil, ili CN; ili c) R9 je CH3, CN ili halo.
6. Spoj prema bilo kojem od zahtjeva 1-5, ili njegova farmaceutski prihvatljiva sol ili stereoizomer, naznačen time što R5 je H.
7. Spoj prema bilo kojem od zahtjeva 1-6, ili njegova farmaceutski prihvatljiva sol ili stereoizomer, naznačen time što: a) G1 je NR6 i G2 je CR7R7; ili b) G1 je CR6R6 i G2 je NR7.
8. Spoj prema zahtjevu 7, ili njegova farmaceutski prihvatljiva sol ili stereoizomer, naznačen time što R6 je H ili C1-6 alkil po izboru supstituiran s 1, 2 ili 3 supstituenta Rb.
9. Spoj prema zahtjevu 7, ili njegova farmaceutski prihvatljiva sol ili stereoizomer, naznačen time što R7 je H ili C1-6 alkil po izboru supstituiran s 1, 2 ili 3 supstituenta Rb.
10. Spoj prema bilo kojem od zahtjeva 1-9, ili njegova farmaceutski prihvatljiva sol ili stereoizomer, naznačen time što: a) svaki Rb supstituent je neovisno odabran iz niza koji sadrži halo, C1-6 alkil, C1-6 haloalkil, C1-6 haloalkoksi, CN, OH, NH2, ORc, C(O)Rc, C(O)NRcRc, i C(O)ORc; ili b) svaki Rb supstituent je neovisno odabran iz niza koji sadrži C1-6 alkil, CN, OH, i C(O)ORc.
11. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol ili stereoizomer, naznačen time što: a) R1, R2 i R3 su svaki neovisno odabrani iz niza koji sadrži H, C1-4 alkil, C3-6 cikloalkil, C2-4 alkenil, C2-4 alkinil, halo, CN, OH, C1-4 alkoksi, C1-4 haloalkil, C1-4 haloalkoksi, NH2, - NH-C1-4 alkil, -N(C1-4 alkil)2, C(O)R10, C(O)NR10R10, C(O)OR10, OC(O)R10, OC(O)NR10R10, NR10C(O)R10, NR10C(O)OR10, NR10S(O)R10, NR10S(O)2R10, NR10S(O)2NR10R10, S(O)R10, S(O)NR10R10, S(O)2R10, i S(O)2NR10R10, pri čemu svaki R10 je neovisno odabran iz niza koji sadrži H i C1-4 alkil po izboru supstituiran s 1 ili 2 skupine neovisno odabrane od halo, OH, CN i C1-4 alkoksi; i pri čemu C1-4 alkil, C3-6 cikloalkil, C2-4 alkenil, C2-4 alkinil i C1-4 alkoksi od R1, R2 i R3 su svaki po izboru supstituirani s 1 ili 2 supstituenta neovisno odabrana iz niza koji sadrži halo, OH, CN i C1-4 alkoksi; R4, R5, R6, R7 i R8 su svaki neovisno odabrani iz niza koji sadrži H, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C1-6 haloalkoksi, CN, NO2, ORa, SRa, C(O)Ra, C(O)NRaRa, C(O)ORa, OC(O)Ra, OC(O)NRaRa, NHRa, NRaRa, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)Ra, NRaS(O)2Ra, NRaS(O)2NRaRa, S(O)Ra, S(O)NRaRa, S(O)2Ra, i S(O)2NRaRa, pri čemu C1-6 alkil, C2-6 alkenil, i C2-6 alkinil od R4, R5, R6, R7 i R8 su svaki po izboru supstituirani s 1, 2, 3, 4 ili 5 supstituenata Rb; ili dva susjedna R8 supstituenta na Cy prstenu, uzeti zajedno s atomima na koje su oni vezani, tvore kondenzirani fenilni prsten, kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten, kondenzirani 5- ili 6-člani heteroarilni prsten ili kondenzirani C3-6 cikloalkilni prsten, pri čemu kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten i kondenzirani 5- ili 6-člani heteroarilni prsten svaki imaju 1-4 heteroatoma kao članove prstena odabrane između N, O i S i pri čemu kondenzirani fenilni prsten, kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten, kondenzirani 5- ili 6-člani heteroarilni prsten i kondenzirani C3-6 cikloalkilni prsten su svaki po izboru supstituirani s 1, 2 ili 3 neovisno odabrana supstituenta Rb; R9 je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C1-6 haloalkoksi, CN, NO2, OR11, SR11, NH2, NHR11, NR11R11, NHOR11, C(O)R11, C(O)NR11R11, C(O)OR11, OC(O)R11, OC(O)NR11R11, NR11C(O)R11, NR11C(O)OR11, NR11C(O)NR11R11, NR11S(O)R11, NR11S(O)2R11, NR11S(O)2NR11R11, S(O)R11, S(O)NR11R11, S(O)2R11, ili S(O)2NR11R11, pri čemu C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, i C1-6 haloalkoksi od R9 su svaki po izboru supstituirani s 1, 2 ili 3 Rb supstituenta; svaki R11 je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, i C2-6 alkinil; svaki Ra je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, i C2-6 alkinil; svaki Rb supstituent je neovisno odabran iz niza koji sadrži halo, C1-6 alkil, C1-6 haloalkil, C1-6 haloalkoksi, CN, OH, NH2, NO2, NHORc, ORc, SRc, C(O)Rc, C(O)NRcRc, C(O)ORc, OC(O)Rc, OC(O)NRcRc, NHRc, NRcRc, NRcC(O)Rc, NRcC(O)ORc, NRcC(O)NRcRc, NRcS(O)Rc, NRcS(O)2Rc, NRcS(O)2NRcRc, S(O)Rc, S(O)NRcRc, S(O)2Rc i S(O)2NRcRc; pri čemu C1-6 alkil, C1-6 haloalkil, i C1-6 haloalkoksi od Rb su svaki dalje po izboru supstituirani s 1-3 neovisno odabrana supstituenta Rd; svaki Rc je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, i C2-6 alkinil, pri čemu C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, i C2-6 alkinil od Rc su svaki po izboru supstituirani s 1, 2 ili 3 supstituenta Rf neovisno odabrana iz niza koji sadrži C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, halo, CN, ORg, SRg, C(O)Rg, C(O)NRgRg, C(O)ORg, OC(O)Rg, OC(O)NRgRg, NHRg, NRgRg, NRgC(O)Rg, NRgC(O)NRgRg, NRgC(O)ORg, S(O)Rg, S(O)NRgRg, S(O)2Rg, NRgS(O)2Rg, NRgS(O)2NRgRg, i S(O)2NRgRg; svaki Rd je neovisno odabran iz niza koji sadrži C1-6 alkil, C1-6 haloalkil, halo, CN, NH2, ORe, SRe, C(O)Re, C(O)NReRe, C(O)ORe, OC(O)Re, OC(O)NReRe, NHRe, NReRe, NReC(O)Re, NReC(O)NReRe, NReC(O)ORe, S(O)Re, S(O)NReRe, S(O)2Re, NReS(O)2Re, NReS(O)2NReRe, i S(O)2NReRe; svaki Re je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil-; svaki Rg je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil-, C3-10 cikloalkil-C1-4 alkil-, (5-10 člani heteroaril)-C1-4 alkil-, i (4-10 člani heterocikloalkil)-C1-4 alkil-; [image] je jednostruka veza ili dvostruka veza kako bi prsten A bio aromatski; i indeks n je cijeli broj 1, 2, 3 ili 4; ili b) R1, R2 i R3 su svaki neovisno odabrani iz niza koji sadrži H, C1-4 alkil, C3-6 cikloalkil, C2-4 alkenil, C2-4 alkinil, halo, CN, OH, C1-4 alkoksi, C1-4 haloalkil, C1-4 haloalkoksi, NH2, - NH-C1-4 alkil, i -N(C1-4 alkil)2; R4, R5, R6, R7 i R8 su svaki neovisno odabrani iz niza koji sadrži H, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C1-6 haloalkoksi, CN, NO2, ORa, SRa, C(O)Ra, C(O)NRaRa, i C(O)ORa, pri čemu C1-6 alkil, C2-6 alkenil, i C2-6 alkinil od R4, R5, R6, R7 i R8 su svaki po izboru supstituirani s 1, 2, 3, 4 ili 5 supstituenata Rb; ili dva susjedna R8 supstituenta na Cy prstenu, uzeti zajedno s atomima na koje su oni vezani, tvore kondenzirani fenilni prsten, kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten, kondenzirani 5- ili 6-člani heteroarilni prsten ili kondenzirani C3-6 cikloalkilni prsten, pri čemu kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten i kondenzirani 5- ili 6-člani heteroarilni prsten svaki imaju 1-4 heteroatoma kao članove prstena odabrane između N, O i S i pri čemu su kondenzirani fenilni prsten, kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten, kondenzirani 5- ili 6-člani heteroarilni prsten i kondenzirani C3-6 cikloalkilni prsten svaki po izboru supstituirani s 1, 2 ili 3 neovisno odabrana supstituenta Rb; R9 je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C1-6 haloalkoksi, CN, NO2, ili NH2, pri čemu C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, i C1-6 haloalkoksi od R9 su svaki po izboru supstituirani s 1, 2 ili 3 supstituenta Rb; svaki Ra je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, i C2-6 alkinil; svaki Rb supstituent je neovisno odabran iz niza koji sadrži halo, C1-6 alkil, C1-6 haloalkil, C1-6 haloalkoksi, CN, OH, NH2, NO2, ORc, SRc, C(O)Rc, C(O)NRcRc, C(O)ORc, NHRc, NRcRc, i NRcC(O)Rc; pri čemu C1-6 alkil, C1-6 haloalkil, i C1-6 haloalkoksi od Rb su svaki dalje po izboru supstituirani s 1-3 neovisno odabrana supstituenta Rd; svaki Rc je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, i C2-6 alkinil; svaki Rd je neovisno odabran iz niza koji sadrži C1-6 alkil, C1-6 haloalkil, halo, CN, NH2, ORe, SRe, C(O)Re, C(O)NReRe, C(O)ORe, NHRe, NReRe, i NReC(O)Re; svaki Re je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, i C2-6 alkinil; [image] je jednostruka veza ili dvostruka veza kako bi prsten A bio aromatski; i indeks n je cijeli broj 1 ili 2; ili c) R1, R2 i R3 su svaki neovisno odabrani iz niza koji sadrži H, C1-4 alkil, C2-4 alkenil, C2-4 alkinil, halo, CN, OH, C1-4 alkoksi, C1-4 haloalkil, i C1-4 haloalkoksi; R4, R5, R6, R7 i R8 su svaki neovisno odabrani iz niza koji sadrži H, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C1-6 haloalkoksi, CN, NO2, ORa, i C(O)ORa, pri čemu su C1-6 alkil, C2-6 alkenil, i C2-6 alkinil od R4, R5, R6, R7 i R8 svaki po izboru supstituirani s 1 ili 2 supstituenta Rb; ili dva susjedna R8 supstituenta na Cy prstenu, uzeti zajedno s atomima na koje su oni vezani, tvore kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten, ili kondenzirani 5- ili 6-člani heteroarilni prsten, pri čemu kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten i kondenzirani 5- ili 6-člani heteroarilni prsten svaki imaju 1-4 heteroatoma kao članove prstena odabrane između N, O i S i pri čemu su kondenzirani 5-, 6- ili 7-člani heterocikloalkilni prsten i kondenzirani 5- ili 6-člani heteroarilni prsten svaki po izboru supstituirani s 1 ili 2 neovisno odabrana supstituenta Rb; R9 je halo, C1-6 alkil, ili CN; svaki Ra je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, i C2-6 alkinil; svaki Rb supstituent je neovisno odabran iz niza koji sadrži halo, C1-6 alkil, C1-6 haloalkil, C1-6 haloalkoksi, CN, OH, NH2, ORc, C(O)Rc, C(O)NRcRc, i C(O)ORc; svaki Rc je neovisno odabran iz niza koji sadrži H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, i C2-6 alkinil; [image] je jednostruka veza ili dvostruka veza kako bi prsten A bio aromatski; i indeks n je cijeli broj 1 ili 2.
12. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što je spoj odabran iz niza koji sadrži: N-[2-cijano-3-(2,3-dihidro-1,4-benzodioksin-6-il)fenil]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-cijanobifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-[2-cijano-3-(1-metil-1H-indazol-4-il)fenil]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-cijano-2'-fluorbifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-cijano-2'-fluor-3'-metoksibifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-[2-cijano-3-(2,3-dihidro-1-benzofuran-6-il)fenil]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-cijano-3-cikloheks-1-en-1-ilfenil)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-cijano-3-cikloheksilfenil)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-cijano-2',6'-difluorbifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-[2-cijano-3-(2,3-dihidro-1,4-benzodioksin-6-il)fenil]-4,5,6,7-tetrahidropirazolo[1,5-a]pirazin-2-karboksamid; N-[2-cijano-3-(2,3-dihidro-1,4-benzodioksin-6-il)fenil]-5-(2-hidroksietil)-4,5,6,7-tetrahidropirazolo[1,5-a]pirazin-2-karboksamid; N-[2-cijano-3-(2,3-dihidro-1,4-benzodioksin-6-il)fenil]-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamid; N-(2-cijano-3-(2,3-dihidrobenzo[b][1,4]dioksin-6-il)fenil)-5-(2-hidroksietil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamid; N-[2-cijano-3-(2,3-dihidro-1,4-benzodioksin-6-il)fenil]-5,6,7,8-tetrahidro[1,2,4]triazolo[1,5-a]pirazin-2-karboksamid; N-(2,3'-dicijano-2'-fluorbifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-cijano-3'-metoksibifenil-3-il)-4,5,6,7-tetrahidrotiazolo[5,4-c]piridin-2-karboksamid; N-(2-cijano-3'-fluor-5'-metoksibifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2'-kloro-2-cijanobifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-cijano-2'-fluor-3'-metoksibifenil-3-il)-5,6,7,8-tetrahidroimidazo[1,2-a]pirazin-2-karboksamid; N-[3-(2,3-dihidro-1,4-benzodioksin-6-il)-2-metilfenil]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2'-fluor-3'-metoksi-2-metilbifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2'-fluor-3'-metoksi-2-metilbifenil-3-il)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamid; N-[2-metil-3-(1-metil-1H-indazol-4-il)fenil]-4,5,6, 7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-[2'-fluor-3'-(hidroksimetil)-2-metilbifenil-3-il]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-[3-(1H-indazol-4-il)-2-metilfenil]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-metilbifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; 5-(2-hidroksietil)-N-(2-metilbifenil-3-il)-4,5,6,7-tetrahidrotiazolo[5,4-c]piridin-2-karboksamid; 2-(2-(2-metilbifenil-3-ilkarbamoil)-6,7-dihidrotiazolo[5,4-c]piridin-5(4H)-il)octena kiselina; N-[2-metil-3-(2-metil-2H-indazol-6-il)fenil]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2'-cijano-2-metilbifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-[2'-(cijanometil)-2-metilbifenil-3-il]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-kloro-2'-fluor-3'-metoksibifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-klorobifenil-3-il)-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-[2-kloro-3-(2,3-dihidro-1,4-benzodioksin-6-il)fenil]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-kloro-3-(1-metil-1H-indazol-4-il)fenil)-4,5,6,7-tetrahidrotiazolo[5,4-c]piridin-2-karboksamid; N-[3-(2,3-dihidro-1,4-benzodioksin-6-il)-5-fluor-2-metilfenil]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-[2-(2,3-dihidro-1,4-benzodioksin-6-il)-3-metilpiridin-4-il]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-[5-(2,3-dihidro-1,4-benzodioksin-6-il)-4-metilpiridin-3-il]-4,5,6,7-tetrahidro[1,3]tiazolo[5,4-c]piridin-2-karboksamid; N-(2-cijano-2'-fluor-3'-metoksibifenil-3-il)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamid; N-(2-cijano-2'-fluor-3'-metoksibifenil-3-il)-5-(2-hidroksietil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamid; (2-{[(2-cijano-2'-fluor-3'-metoksibifenil-3-il)amino]karbonil}-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)octena kiselina; i N-(2-cijano-3-(1-metil-1H-indazol-4-il)fenil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamid.
13. Farmaceutski pripravak koji sadrži spoj prema bilo kojem od zahtjeva 1-11, ili njegovu farmaceutski prihvatljivu sol ili stereoizomer, ili spoj prema zahtjevu 12, ili njegovu farmaceutski prihvatljivu sol, i najmanje jedan farmaceutski prihvatljiv nosač ili pomoćnu tvar.
14. Spoj prema bilo kojem od zahtjeva 1-11, ili njegova farmaceutski prihvatljiva sol ili stereoizomer; spoj prema zahtjevu 12, ili njegova farmaceutski prihvatljiva sol; ili pripravak prema zahtjevu 13, za upotrebu u postupku liječenja bolesti ili poremećaja povezanog s inhibicijom interakcije PD-1/PD-L1, pri čemu je bolest ili poremećaj rak ili infekcija.
15. Spoj, sol, stereoizomer ili pripravak za upotrebu prema zahtjevu 14, naznačen time što je bolest ili poremećaj infekcija, a infekcija je virusna infekcija.
16. Spoj, sol, stereoizomer ili pripravak za upotrebu prema zahtjevu 14, naznačen time što je bolest ili poremećaj rak.
17. Spoj, sol, stereoizomer ili pripravak za upotrebu prema zahtjevu 16, naznačen time što: (a) rak je odabran od raka kostiju, raka kože, raka glave ili vrata, intraokularnog malignog melanoma, raka maternice, raka jajnika, raka rektuma, raka analnog područja, raka želuca, raka testisa, karcinoma jajovoda, karcinoma endometrija, karcinoma grlića maternice, karcinoma vagine, karcinoma vulve, ne-Hodgkinovog limfom, raka jednjaka, raka tankog crijeva, raka endokrinog sustava, raka štitnjače, raka paratireoidne žlijezde, raka nadbubrežne žlijezde, sarkoma mekog tkiva, raka uretre, raka penisa, kroničnih ili akutnih leukemija, solidnih tumora dječje dobi, limfocitnog limfoma, raka mokraćnog mjehura, karcinoma bubrežne zdjelice, neoplazme središnjeg živčanog sustava (SŽS), primarnog limfoma središnjeg živčanog sustava (SŽS), angiogeneze tumora, tumora osi kralježnice, glioma moždanog debla, adenoma hipofize, Kaposijevog sarkoma, epidermoidnog karcinoma, raka pločastih stanica, T-staničnog limfoma, karcinoma uzrokovanih okolišem uključujući one izazvane azbestom, melanoma, metastatskog malignog melanoma, raka bubrega, svijetlostaničnog karcinoma, prostate raka prostate, adenokarcinoma prostate otpornog na hormone, raka dojke, raka debelog crijeva, raka pluća, raka pluća nemalih stanica, solidnih tumora, raka endometrija, raka jetre, raka gušterače, raka želuca, raka štitnjače, glioblastoma, sarkoma, hematoloških karcinoma, limfoma, leukemije, akutne limfoblastične leukemije (ALL), akutne mijeloične leukemije (AML), kronične limfocitne leukemije (CLL), kronične mijeloične leukemije (CML), difuznog limfoma velikih B stanica (DLBCL), limfoma plaštenih stanica, ne-Hodgkinovog limfoma, relapsirajućeg ili refraktornog ne-Hodgkinovog limfoma (NHL), recidivirajućeg folikularnog limfoma, Hodgkinovog limfoma, i multiplog mijeloma; ili (b) rak je metastatski rak koji eksprimira PD-L1; ili (c) rak je rak pluća; ili (d) rak je rak pluća nemalih stanica; ili (e) rak je rak bubrega; ili (f) rak je rak jetre; ili (g) rak je melanom; ili (h) rak je rak mokraćnog mjehura ili (i) rak je rak uretre; ili (j) rak je rak bubrega; ili (k) rak je svijetlostanični karcinom bubrežnih stanica.
18. Spoj prema bilo kojem od zahtjeva 1-11, ili njegova farmaceutski prihvatljiva sol ili stereoizomer; spoj prema zahtjevu 12, ili njegova farmaceutski prihvatljiva sol; ili pripravak prema zahtjevu 13, za upotrebu u postupku poboljšanja, stimuliranja i/ili povećanja imunološkog odgovora kod pacijenta.
HRP20221030TT 2016-06-20 2017-06-19 Heterociklički spojevi kao imunomodulatori HRP20221030T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662352485P 2016-06-20 2016-06-20
US201662396353P 2016-09-19 2016-09-19
PCT/US2017/038120 WO2017222976A1 (en) 2016-06-20 2017-06-19 Heterocyclic compounds as immunomodulators
EP17734589.9A EP3472167B1 (en) 2016-06-20 2017-06-19 Heterocyclic compounds as immunomodulators

Publications (1)

Publication Number Publication Date
HRP20221030T1 true HRP20221030T1 (hr) 2022-11-11

Family

ID=59258383

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20221030TT HRP20221030T1 (hr) 2016-06-20 2017-06-19 Heterociklički spojevi kao imunomodulatori

Country Status (31)

Country Link
US (4) US20170362253A1 (hr)
EP (2) EP4137489A1 (hr)
JP (2) JP7000357B2 (hr)
KR (1) KR102685249B1 (hr)
CN (1) CN109890819B (hr)
AU (2) AU2017281285C1 (hr)
BR (1) BR112018076534A2 (hr)
CL (1) CL2018003701A1 (hr)
CO (1) CO2019000386A2 (hr)
DK (1) DK3472167T3 (hr)
EC (1) ECSP19003773A (hr)
ES (1) ES2927984T3 (hr)
HR (1) HRP20221030T1 (hr)
HU (1) HUE060256T2 (hr)
IL (1) IL263825B (hr)
LT (1) LT3472167T (hr)
MD (1) MD3472167T2 (hr)
MX (2) MX389513B (hr)
MY (1) MY197280A (hr)
PE (1) PE20190731A1 (hr)
PH (1) PH12018502710A1 (hr)
PL (1) PL3472167T3 (hr)
PT (1) PT3472167T (hr)
RS (1) RS63673B1 (hr)
SG (2) SG11201811414TA (hr)
SI (1) SI3472167T1 (hr)
SM (1) SMT202200392T1 (hr)
TW (1) TWI771305B (hr)
UA (1) UA125391C2 (hr)
WO (1) WO2017222976A1 (hr)
ZA (1) ZA202405294B (hr)

Families Citing this family (178)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2017070089A1 (en) 2015-10-19 2017-04-27 Incyte Corporation Heterocyclic compounds as immunomodulators
SG10202004618TA (en) 2015-11-19 2020-06-29 Incyte Corp Heterocyclic compounds as immunomodulators
MA44075A (fr) 2015-12-17 2021-05-19 Incyte Corp Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1
AU2016379372A1 (en) 2015-12-22 2018-08-02 Incyte Corporation Heterocyclic compounds as immunomodulators
AR108396A1 (es) 2016-05-06 2018-08-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
WO2017205464A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
HUE060256T2 (hu) 2016-06-20 2023-02-28 Incyte Corp Heterociklusos vegyületek mint immunmodulátorok
US10639284B2 (en) 2016-06-27 2020-05-05 Chemocentryx, Inc. Immunomodulator compounds
EP3484866B1 (en) 2016-07-14 2022-09-07 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018044783A1 (en) 2016-08-29 2018-03-08 Incyte Corporation Heterocyclic compounds as immunomodulators
KR20230010826A (ko) 2016-10-14 2023-01-19 프리시젼 바이오사이언시스 인코포레이티드 B형 간염 바이러스 게놈 내의 인식 서열에 대해 특이적인 조작된 메가뉴클레아제
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
JP7101678B2 (ja) 2016-12-22 2022-07-15 インサイト・コーポレイション 免疫調節剤としての複素環式化合物
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
LT3558990T (lt) * 2016-12-22 2022-12-27 Incyte Corporation Tetrahidroimidazo[4,5-c]piridino dariniai kaip pd-l1 internalizavimo induktoriai
US20180179202A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
EP3567049A4 (en) 2016-12-28 2020-08-26 Green Cross Lab Cell Corporation CHEMERICAL ANTIGENIC RECEPTOR AND NATURAL KILLER CELLS EXPRESSING THE SAME
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
WO2018200571A1 (en) 2017-04-25 2018-11-01 Arbutus Biopharma Corporation Substituted 2,3-dihydro-1h-indene analogs and methods using same
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
US10919852B2 (en) 2017-07-28 2021-02-16 Chemocentryx, Inc. Immunomodulator compounds
US10392405B2 (en) 2017-08-08 2019-08-27 Chemocentryx, Inc. Macrocyclic immunomodulators
US11649294B2 (en) 2017-11-14 2023-05-16 GC Cell Corporation Anti-HER2 antibody or antigen-binding fragment thereof, and chimeric antigen receptor comprising same
KR102774451B1 (ko) 2017-11-14 2025-02-28 앱클론(주) 항-her2 항체 또는 그의 항원 결합 단편, 및 이를 포함하는 키메라 항원 수용체
EP3728283B1 (en) 2017-12-20 2023-11-22 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
WO2019123339A1 (en) 2017-12-20 2019-06-27 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
WO2019149183A1 (zh) * 2018-02-05 2019-08-08 上海和誉生物医药科技有限公司 一种联芳基衍生物、其制备方法和在药学上的应用
CR20200347A (es) 2018-02-13 2020-09-23 Gilead Sciences Inc Inhibidores pd-1/pd-l1
US10568874B2 (en) 2018-02-22 2020-02-25 Chemocentryx, Inc. Indane-amines as PD-L1 antagonists
JP7050165B2 (ja) 2018-02-26 2022-04-07 ギリアード サイエンシーズ， インコーポレイテッド Ｈｂｖ複製阻害剤としての置換ピロリジン化合物
TWI877770B (zh) 2018-02-27 2025-03-21 美商英塞特公司 作為a2a / a2b抑制劑之咪唑并嘧啶及三唑并嘧啶
US12083118B2 (en) 2018-03-29 2024-09-10 Arbutus Biopharma Corporation Substituted 1,1′-biphenyl compounds, analogues thereof, and methods using same
SMT202500157T1 (it) * 2018-03-30 2025-05-12 Incyte Corp Composti eterociclici come immunomodulatori
JP2021520342A (ja) * 2018-04-03 2021-08-19 ベータ ファーマシューティカルズ カンパニー リミテッド 免疫調節物質、組成物及びそれらの方法
US10870691B2 (en) 2018-04-05 2020-12-22 Gilead Sciences, Inc. Antibodies and fragments thereof that bind hepatitis B virus protein X
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 ２，２，─環二核苷酸
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
US11142750B2 (en) 2018-04-12 2021-10-12 Precision Biosciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the Hepatitis B virus genome
TWI712412B (zh) 2018-04-19 2020-12-11 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
US20190359645A1 (en) 2018-05-03 2019-11-28 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotides comprising carbocyclic nucleotide
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
HUE061503T2 (hu) * 2018-05-11 2023-07-28 Incyte Corp Tetrahidro-imidazo[4,5-C]piridin-származékok mint PD-L1 immunmodulátorok
EP3810610A1 (en) 2018-05-18 2021-04-28 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
WO2019232319A1 (en) 2018-05-31 2019-12-05 Peloton Therapeutics, Inc. Compositions and methods for inhibiting cd73
WO2020010197A1 (en) 2018-07-05 2020-01-09 Incyte Corporation Fused pyrazine derivatives as a2a / a2b inhibitors
SG11202012425QA (en) 2018-07-13 2021-01-28 Gilead Sciences Inc Pd-1/pd-l1 inhibitors
WO2020028097A1 (en) 2018-08-01 2020-02-06 Gilead Sciences, Inc. Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid
FI3851436T3 (fi) 2018-09-10 2024-09-03 Kaken Pharma Co Ltd Uusi heteroaromaattinen amidijohdannainen ja sitä sisältävä lääke
WO2020068729A1 (en) 2018-09-25 2020-04-02 Incyte Corporation Pyrazolo[4,3-d]pyrimidine compounds as alk2 abd/or fgfr modulators
US12331320B2 (en) 2018-10-10 2025-06-17 The Research Foundation For The State University Of New York Genome edited cancer cell vaccines
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
WO2020086556A1 (en) 2018-10-24 2020-04-30 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
US11203591B2 (en) 2018-10-31 2021-12-21 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds
WO2020092528A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
AU2019373702A1 (en) 2018-11-02 2021-06-24 Shanghai Maxinovel Pharmaceuticals Co., Ltd. Diphenyl-like compound, intermediate thereof, preparation method therefor, pharmaceutical composition thereof and uses thereof
CA3124088A1 (en) 2018-12-20 2020-06-25 Incyte Corporation Imidazopyridazine and imidazopyridine compounds as inhibitors of activin receptor-like kinase-2
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
EP3919478A4 (en) * 2019-02-02 2022-12-07 Shanghai Fosun Pharmaceutical Industrial Development Co., Ltd. VINYLPYRIDINE CARBOXAMIDE COMPOUND USEFUL AS A PD-L1 IMMUNOMODULATOR
CN112752749B (zh) 2019-02-02 2021-07-16 南京明德新药研发有限公司 作为pd-l1免疫调节剂的氟乙烯基苯甲酰胺基化合物
PH12021551976A1 (en) 2019-02-15 2022-07-04 Incyte Corp Cyclin-dependent kinase 2 biomarkers and uses thereof
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
WO2020178770A1 (en) 2019-03-07 2020-09-10 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
EP3934757B1 (en) 2019-03-07 2023-02-22 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 2'3'-cyclic dinucleotides and prodrugs thereof
WO2020178768A1 (en) 2019-03-07 2020-09-10 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
EP3943083A4 (en) 2019-03-22 2023-06-07 Guangzhou Maxinovel Pharmaceuticals Co., Ltd. SMALL MOLECULE PD-1/PD-L1 INHIBITOR, PHARMACEUTICAL COMPOSITION THEREOF WITH PD-L1 ANTIBODY, AND USES THEREOF
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
TWI751516B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202212339A (zh) 2019-04-17 2022-04-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
WO2020232256A1 (en) * 2019-05-15 2020-11-19 Chemocentryx, Inc. Triaryl compounds for treatment of pd-l1 diseases
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
WO2020257549A2 (en) 2019-06-20 2020-12-24 Chemocentryx, Inc. Compounds for treatment of pd-l1 diseases
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
BR112021025888A2 (pt) 2019-07-10 2022-04-26 Chemocentryx Inc Indanos como inibidores de pd-l1
US20220257619A1 (en) 2019-07-18 2022-08-18 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
JP7665593B2 (ja) 2019-08-09 2025-04-21 インサイト・コーポレイション Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩
CA3150681A1 (en) 2019-08-14 2021-02-18 Incyte Corporation Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2021034804A1 (en) 2019-08-19 2021-02-25 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
DK4037708T3 (da) 2019-09-30 2024-09-30 Gilead Sciences Inc HBV-vacciner og fremgangsmåder til at behandle HBV
PE20221038A1 (es) 2019-09-30 2022-06-17 Incyte Corp Compuestos de pirido[3,2-d] pirimidina como inmunomoduladores
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11851426B2 (en) 2019-10-11 2023-12-26 Incyte Corporation Bicyclic amines as CDK2 inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7736678B2 (ja) 2019-10-16 2025-09-09 ケモセントリックス，インコーポレイティド Ｐｄ－ｌ１疾患の処置のためのヘテロアリール－ビフェニルアミド
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
ES3064674T3 (en) 2019-10-16 2026-04-28 Chemocentryx Inc Heteroaryl-biphenyl amines for the treatment of pd-l1 diseases
CA3160131A1 (en) 2019-11-11 2021-05-20 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
CN112812113B (zh) * 2019-11-15 2022-09-20 杭州和正医药有限公司 免疫调节化合物、组合物及其应用
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Ｆｇｆｒ阻害剤の誘導体
DK4069729T3 (da) 2019-12-06 2025-04-07 Prec Biosciences Inc Optimerede, modificerede meganukleaser med specificitet for en genkendelsessekvens i hepatitis b-virusgenomet
CN110950886A (zh) * 2019-12-13 2020-04-03 苏州莱克施德药业有限公司 一种合成1-甲基-咪唑-2-甲酸甲酯衍生物的方法
US20210205311A1 (en) 2020-01-03 2021-07-08 Incyte Corporation Combination Therapy Comprising A2A/A2B and PD-1/PD-L1 Inhibitors
WO2021136354A1 (zh) 2020-01-03 2021-07-08 上海翰森生物医药科技有限公司 联苯类衍生物抑制剂、其制备方法和应用
TWI867137B (zh) * 2020-01-07 2024-12-21 大陸商上海和譽生物醫藥科技有限公司 聯苯基氟代雙鍵衍生物及其製備方法和在藥學上的應用
US20210269434A1 (en) 2020-01-10 2021-09-02 Incyte Corporation Tricyclic compounds as inhibitors of kras
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021150613A1 (en) 2020-01-20 2021-07-29 Incyte Corporation Spiro compounds as inhibitors of kras
CN114650993B (zh) * 2020-01-21 2024-11-26 上海华汇拓医药科技有限公司 一种pd-1/pd-l1抑制剂及其制备方法和用途
US20210253582A1 (en) 2020-02-06 2021-08-19 Incyte Corporation Salts and solid forms and processes of preparing a pi3k inhibitor
WO2021178779A1 (en) 2020-03-06 2021-09-10 Incyte Corporation Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors
WO2021188959A1 (en) 2020-03-20 2021-09-23 Gilead Sciences, Inc. Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same
AU2021254794A1 (en) 2020-04-16 2022-12-15 Incyte Corporation Fused tricyclic KRAS inhibitors
KR20230041654A (ko) 2020-05-05 2023-03-24 테온 테라퓨틱스, 인크. 칸나비노이드 수용체 유형 2 (cb2) 조정제 및 그의 용도
US11739102B2 (en) 2020-05-13 2023-08-29 Incyte Corporation Fused pyrimidine compounds as KRAS inhibitors
CA3184811A1 (en) 2020-06-12 2021-12-16 Incyte Corporation Imidazopyridazine compounds with activity as alk2 inhibitors
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
CR20230057A (es) 2020-07-02 2023-08-15 Incyte Corp Compuestos tríciclicos de urea como inhibidores de jak2 v617f
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
US11999752B2 (en) 2020-08-28 2024-06-04 Incyte Corporation Vinyl imidazole compounds as inhibitors of KRAS
JP7810700B2 (ja) 2020-09-09 2026-02-03 ベイジン マキシノベル ファーマシューティカルズ カンパニー リミテッド 芳香族エチレン系化合物、その製造方法、中間体、医薬組成物及びその使用
US11767320B2 (en) 2020-10-02 2023-09-26 Incyte Corporation Bicyclic dione compounds as inhibitors of KRAS
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式
CR20230230A (es) 2020-11-06 2023-07-27 Incyte Corp Proceso para hacer un inhibidor de pd-1/pdl1 y sales y formas cristalinas del mismo
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
TW202241441A (zh) 2020-12-29 2022-11-01 美商英塞特公司 包含ａ２ａ／ａ２ｂ抑制劑、ｐｄ－１／ｐｄ－ｌ１抑制劑及抗ｃｄ７３抗體之組合療法
AR125273A1 (es) 2021-02-25 2023-07-05 Incyte Corp Lactamas espirocíclicas como inhibidores de jak2 v617f
WO2022204112A1 (en) 2021-03-22 2022-09-29 Incyte Corporation Imidazole and triazole kras inhibitors
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
WO2022241134A1 (en) 2021-05-13 2022-11-17 Gilead Sciences, Inc. COMBINATION OF A TLR8 MODULATING COMPOUND AND ANTI-HBV siRNA THERAPEUTICS
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TWI910028B (zh) 2021-06-11 2025-12-21 美商基利科學股份有限公司 Mcl-1抑制劑與抗癌劑之組合
US11931424B2 (en) 2021-06-11 2024-03-19 Gilead Sciences, Inc. Combination MCL-1 inhibitors with anti-body drug conjugates
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
MX2023014762A (es) 2021-06-23 2024-01-15 Gilead Sciences Inc Compuestos moduladores de diacilglicerol quinasa.
AU2022299051B2 (en) 2021-06-23 2025-03-13 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
JP7651018B2 (ja) 2021-06-23 2025-03-25 ギリアード サイエンシーズ， インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
JP7686091B2 (ja) 2021-06-23 2025-05-30 ギリアード サイエンシーズ， インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
MX2024000357A (es) 2021-07-07 2024-02-12 Incyte Corp Compuestos triciclicos como inhibidores de homologo de oncogen viral de sarcoma de rata kirsten (kras).
WO2023287896A1 (en) 2021-07-14 2023-01-19 Incyte Corporation Tricyclic compounds as inhibitors of kras
US12441742B2 (en) 2021-08-31 2025-10-14 Incyte Corporation Naphthyridine compounds as inhibitors of KRAS
TW202325306A (zh) 2021-09-02 2023-07-01 美商天恩治療有限公司 改良免疫細胞之生長及功能的方法
WO2023049697A1 (en) 2021-09-21 2023-03-30 Incyte Corporation Hetero-tricyclic compounds as inhibitors of kras
CA3234375A1 (en) 2021-10-01 2023-04-06 Incyte Corporation Pyrazoloquinoline kras inhibitors
CA3235146A1 (en) 2021-10-14 2023-04-20 Incyte Corporation Quinoline compounds as inhibitors of kras
WO2023081730A1 (en) 2021-11-03 2023-05-11 Teon Therapeutics, Inc. 4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide derivatives as cannabinoid cb2 receptor modulators for the treatment of cancer
MX2024006113A (es) 2021-11-22 2024-07-29 Incyte Corp Terapia de combinación que comprende un inhibidor del receptor del factor de crecimiento de fibroblastos (fgfr) y un inhibidor del sarcoma de rata de kirsten (kras).
WO2023097211A1 (en) 2021-11-24 2023-06-01 The University Of Southern California Methods for enhancing immune checkpoint inhibitor therapy
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
EP4452982A1 (en) 2021-12-22 2024-10-30 Incyte Corporation Salts and solid forms of an fgfr inhibitor and processes of preparing thereof
AU2023235313A1 (en) 2022-03-17 2024-10-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
AU2023284958A1 (en) 2022-06-08 2025-01-02 Incyte Corporation Tricyclic triazolo compounds as dgk inhibitors
US20240101557A1 (en) 2022-07-11 2024-03-28 Incyte Corporation Fused tricyclic compounds as inhibitors of kras g12v mutants
US20260015356A1 (en) 2022-07-14 2026-01-15 Teon Therapeutics, Inc. Adenosine receptor antagonists and uses thereof
US12600722B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
US12600723B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
US20240190876A1 (en) 2022-10-21 2024-06-13 Incyte Corporation Tricyclic Urea Compounds As JAK2 V617F Inhibitors
US20240217989A1 (en) 2022-11-18 2024-07-04 Incyte Corporation Heteroaryl Fluoroalkenes As DGK Inhibitors
TW202428575A (zh) 2023-01-12 2024-07-16 美商英塞特公司 作為ｄｇｋ抑制劑之雜芳基氟代烯烴
JP2026509874A (ja) 2023-03-13 2026-03-25 インサイト・コーポレイション キナーゼ阻害剤としての二環式尿素
US20240390340A1 (en) 2023-04-18 2024-11-28 Incyte Corporation Pyrrolidine kras inhibitors
WO2025043151A2 (en) 2023-08-24 2025-02-27 Incyte Corporation Bicyclic dgk inhibitors
US20250114346A1 (en) 2023-10-09 2025-04-10 Incyte Corporation Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor
WO2025096738A1 (en) 2023-11-01 2025-05-08 Incyte Corporation Kras inhibitors
TW202523667A (zh) 2023-12-05 2025-06-16 美商英塞特公司 作為ｄｇｋ抑制劑之三環三唑并化合物
TW202523304A (zh) 2023-12-06 2025-06-16 美商英塞特公司 包含ｄｇｋ抑制劑及ｐｄ—１／ｐｄ—ｌ１抑制劑之組合療法
US20250195536A1 (en) 2023-12-13 2025-06-19 Incyte Corporation Bicyclooctane kras inhibitors
WO2025240242A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
WO2025240244A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies comprising bulevirtide and lonafarnib for use in the treatment of hepatitis d virus infection
WO2025240243A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with bulevirtide and an inhibitory nucleic acid targeting hepatitis b virus
WO2025240246A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
WO2026035860A1 (en) 2024-08-07 2026-02-12 Teon Therapeutics, Inc. Formulations of adenosine receptor antagonist
US20260069605A1 (en) 2024-09-11 2026-03-12 Incyte Corporation Kras inhibitors

Family Cites Families (359)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3272781A (en) 1963-08-07 1966-09-13 American Potash & Chem Corp Boroureas of phosphinoborine polymers
FR1425700A (fr) 1965-02-22 1966-01-24 Basf Ag Composés formant des complexes métalliques et procédé pour les préparer et les utiliser
US4208328A (en) 1978-04-27 1980-06-17 General Electric Company Alkyl 3,5-dihydroxy-4-(2-benzothiazolyl)benzoates
US4789711A (en) 1986-12-02 1988-12-06 Ciba-Geigy Corporation Multifunctional epoxide resins
DE3828535A1 (de) 1988-08-23 1990-03-08 Basf Ag Benzimidazol-2-carbonsaeureanilide, ihre verwendung als lichtschutzmittel fuer organisches material und mit diesen aniliden stabilisiertes organisches material
US5077164A (en) 1989-06-21 1991-12-31 Minolta Camera Kabushiki Kaisha Photosensitive member containing an azo dye
EP0644460B1 (en) 1993-09-20 1999-12-08 Fuji Photo Film Co., Ltd. Positive working photoresist composition
JP3461397B2 (ja) 1995-01-11 2003-10-27 富士写真フイルム株式会社 ポジ型フオトレジスト組成物
EP0946587A2 (en) 1996-12-16 1999-10-06 Fujisawa Pharmaceutical Co., Ltd. New amide compounds
JPH10316853A (ja) 1997-05-15 1998-12-02 Sumitomo Bakelite Co Ltd 半導体多層配線用層間絶縁膜樹脂組成物及び該絶縁膜の製造方法
AU9781098A (en) 1997-10-02 1999-04-27 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
AU2745899A (en) 1998-03-05 1999-09-20 Nissan Chemical Industries Ltd. Anilide compounds and herbicide
JP2000128987A (ja) 1998-10-28 2000-05-09 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール前駆体及びポリベンゾオキサゾール
JP2000128984A (ja) 1998-10-28 2000-05-09 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール前駆体及び樹脂
JP2000128986A (ja) 1998-10-28 2000-05-09 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール前駆体及びポリベンゾオキサゾール
US6297351B1 (en) 1998-12-17 2001-10-02 Sumitomo Bakelite Company Limited Polybenzoxazole resin and precursor thereof
HUP0104987A3 (en) 1998-12-18 2002-09-30 Axys Pharmaceuticals Inc South Benzimidazole or indole derivatives protease inhibitors, and pharmaceutical compositions containing them
JP2000212281A (ja) 1999-01-27 2000-08-02 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾ―ル前駆体及びポリベンゾオキサゾ―ル樹脂
WO2001007409A1 (en) 1999-07-23 2001-02-01 Astrazeneca Uk Limited Carbazole derivatives and their use as neuropeptide y5 receptor ligands
JP2001114893A (ja) 1999-10-15 2001-04-24 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール樹脂およびその前駆体
US6372907B1 (en) 1999-11-03 2002-04-16 Apptera Corporation Water-soluble rhodamine dye peptide conjugates
JP2001163975A (ja) 1999-12-03 2001-06-19 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール樹脂及びその前駆体
NZ514403A (en) 1999-12-27 2002-10-25 Japan Tobacco Inc Fused-ring compounds and use thereof as drugs
DE50112961D1 (de) 2000-02-01 2007-10-18 Abbott Gmbh & Co Kg Heterozyklische verbindungen und deren anwendung als parp-inhibitoren
US6521618B2 (en) 2000-03-28 2003-02-18 Wyeth 3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
AU2001249679A1 (en) 2000-03-31 2001-10-15 Ortho-Mcneil Pharmaceutical, Inc. Phenyl-substituted imidazopyridines
WO2001081312A2 (en) 2000-04-24 2001-11-01 Merck Frosst Canada & Co. Method of treatment using phenyl and biaryl derivatives as prostaglandin e inhibitors and compounds useful therefore
KR100786927B1 (ko) 2000-06-28 2007-12-17 스미스클라인비이참피이엘시이 습식 분쇄방법
WO2002014321A1 (en) 2000-08-11 2002-02-21 The Regents Of The University Of California Use of stat-6 inhibitors as therapeutic agents
US20040058938A1 (en) 2000-12-13 2004-03-25 Oliver Cullmann Use of substituted imidazoazines, novel imidazoazines, methods for the production thereof, and agents containing these compounds
ATE301653T1 (de) 2000-12-15 2005-08-15 Glaxo Group Ltd Pyrazolopyridine
SE0100567D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
DE60204674T2 (de) 2001-03-14 2006-05-18 Eli Lilly And Co., Indianapolis Retinoid x rezeptormodulatoren
WO2002078700A1 (en) 2001-03-30 2002-10-10 Smithkline Beecham Corporation Pyralopyridines, process for their preparation and use as therapteutic compounds
ES2266487T3 (es) 2001-04-10 2007-03-01 Smithkline Beecham Corporation Compuestos de pirazolopirina antivirales.
JP2002316966A (ja) 2001-04-19 2002-10-31 Ueno Seiyaku Oyo Kenkyusho:Kk ビナフトール誘導体およびその製法
ATE296826T1 (de) 2001-04-27 2005-06-15 Smithkline Beecham Corp Pyrazolo(1,5)pyridinderivate
AR035543A1 (es) 2001-06-26 2004-06-16 Japan Tobacco Inc Agente terapeutico para la hepatitis c que comprende un compuesto de anillo condensado, compuesto de anillo condensado, composicion farmaceutica que lo comprende, compuestos de benzimidazol, tiazol y bifenilo utiles como intermediarios para producir dichos compuestos, uso del compuesto de anillo con
US20040214834A1 (en) 2001-09-07 2004-10-28 Kristjan Gudmunsson Pyrazolo-pyridines for the treatment of herpes infections
TWI320039B (en) 2001-09-21 2010-02-01 Lactam-containing compounds and derivatives thereof as factor xa inhibitors
US20030143199A1 (en) 2001-10-09 2003-07-31 Carson Dennis A. Use of STAT-6 inhibitors as therapeutic agents
WO2003030901A1 (en) 2001-10-09 2003-04-17 Pharmacia & Upjohn Company Arylsulphonyl-substituted tetrahydro- and hexahydro-carbazoles as 5-ht-6 receptor ligands
CA2466279A1 (en) 2001-11-13 2003-05-22 Dana-Farber Cancer Institute, Inc. Agents that modulate immune cell activation and methods of use thereof
JP4024579B2 (ja) 2002-01-22 2007-12-19 住友ベークライト株式会社 プラスチック光導波路用材料及び光導波路
KR20040099425A (ko) 2002-04-11 2004-11-26 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 ｃ형 간염 바이러스 ｎｓ3-ｎｓ4프로테아제의 억제제
US7662826B2 (en) 2002-04-23 2010-02-16 Shionogi & Co., Ltd. Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same
AU2003252478A1 (en) 2002-07-10 2004-02-02 Ono Pharmaceutical Co., Ltd. Ccr4 antagonist and medicinal use thereof
AU2003249244A1 (en) 2002-07-15 2004-02-02 Combinatorx, Incorporated Methods for the treatment of neoplasms
JP2004059761A (ja) 2002-07-30 2004-02-26 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール樹脂、その前駆体及びこれらを用いた光導波路材料並びに光導波路
EP1547996A4 (en) 2002-08-30 2006-08-02 Bf Res Inst Inc DIAGNOSTIC PROBES AND REMEDIES FOR DISEASES IN WHICH PRION PROTEIN IS ACCUMULATED, AND ANIMAL FEVERING FOR PRION PROTEIN
JP2004091369A (ja) * 2002-08-30 2004-03-25 Sumitomo Pharmaceut Co Ltd 新規ビフェニル化合物
JP2006504728A (ja) 2002-10-03 2006-02-09 スミスクライン ビーチャム コーポレーション ピラソロピリジン誘導体系治療用化合物
EP1551842A1 (en) 2002-10-15 2005-07-13 Smithkline Beecham Corporation Pyradazine compounds as gsk-3 inhibitors
CN101899114A (zh) 2002-12-23 2010-12-01 惠氏公司 抗pd-1抗体及其用途
KR100624406B1 (ko) 2002-12-30 2006-09-18 삼성에스디아이 주식회사 비페닐 유도체 및 이를 채용한 유기 전계 발광 소자
US7320989B2 (en) 2003-02-28 2008-01-22 Encysive Pharmaceuticals, Inc. Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
US7078419B2 (en) 2003-03-10 2006-07-18 Boehringer Ingelheim Pharmaceuticals, Inc. Cytokine inhibitors
TW200505902A (en) 2003-03-20 2005-02-16 Schering Corp Cannabinoid receptor ligands
JP4595288B2 (ja) 2003-03-25 2010-12-08 住友ベークライト株式会社 ポリベンゾオキサゾール樹脂、その前駆体及びこれらを用いた光導波路材料並びに光導波路
OA13154A (en) 2003-04-11 2006-12-13 Glenmark Pharmaceuticals Sa Novel heterocyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them.
JP2005002330A (ja) 2003-05-19 2005-01-06 Sumitomo Electric Ind Ltd 光学樹脂材料、光学素子、光モジュール、フッ素化ポリマー前駆体及びフッ素化ポリマー
CL2004001120A1 (es) 2003-05-19 2005-04-15 Irm Llc Compuestos derivados de amina sustituidas con heterociclos, inmunosupresores; composicion farmaceutica; y uso para tratar enfermedades mediadas por interacciones de linfocito, tales como enfermedades autoinmunes, inflamatorias, infecciosas, cancer.
US7405295B2 (en) 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US20060183746A1 (en) 2003-06-04 2006-08-17 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
WO2005005429A1 (en) 2003-06-30 2005-01-20 Cellular Genomics, Inc. Certain heterocyclic substituted imidazo[1,2-a]pyrazin-8-ylamines and methods of inhibition of bruton’s tyrosine kinase by such compounds
WO2005007628A1 (en) 2003-07-11 2005-01-27 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives as cannabinoid receptor modulators
JP5001650B2 (ja) 2003-07-11 2012-08-15 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング ベンズイミダゾールカルボキサミド
JPWO2005012221A1 (ja) 2003-08-04 2006-09-14 小野薬品工業株式会社 ジフェニルエーテル化合物、その製造方法および用途
WO2005014543A1 (ja) 2003-08-06 2005-02-17 Japan Tobacco Inc. 縮合環化合物及びそのｈｃｖポリメラーゼ阻害剤としての利用
US7504401B2 (en) 2003-08-29 2009-03-17 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
WO2005023761A2 (en) 2003-09-11 2005-03-17 Kemia, Inc. Cytokine inhibitors
AU2004279427B2 (en) 2003-10-08 2008-07-03 Irm Llc Compounds and compositions as protein kinase inhibitors
US20070099938A1 (en) 2003-10-24 2007-05-03 Ono Pharmaceutical Co., Ltd. Antistress drug and medical use thereof
WO2005047290A2 (en) 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
JP2007534652A (ja) 2003-12-23 2007-11-29 ビーエーエスエフ　アクチェンゲゼルシャフト ３−トリフルオロメチルピコリン酸アニリドおよび殺菌剤としてのその使用
CA2555402A1 (en) 2004-02-12 2005-09-01 Celine Bonnefous Bipyridyl amides as modulators of metabotropic glutamate receptor-5
EP1717238A4 (en) 2004-02-16 2008-03-05 Daiichi Seiyaku Co FUNGICIDES HETEROCYCLIC COMPOUNDS
GB0403864D0 (en) 2004-02-20 2004-03-24 Ucl Ventures Modulator
JP2005248082A (ja) 2004-03-05 2005-09-15 Sumitomo Electric Ind Ltd ポリベンゾオキサゾール樹脂前駆体の製造方法およびポリベンゾオキサゾール樹脂の製造方法
WO2005086808A2 (en) 2004-03-08 2005-09-22 The University Of North Carolina At Chapel Hill NOVEL DICATIONIC IMIDAZO[1,2-a]PYRIDINES AND 5,6,7,8-TETRAHYDRO-IMIDAZO[1,2a]PYRIDINES AS ANTIPROTOZOAL AGENTS
US20050250820A1 (en) 2004-03-08 2005-11-10 Amgen Inc. Therapeutic modulation of PPARgamma activity
US7423147B2 (en) 2004-03-31 2008-09-09 Janssen Pharmaceutical, N.V. Pyridine compounds as histamine H3 modulators
JP2005290301A (ja) 2004-04-02 2005-10-20 Sumitomo Electric Ind Ltd ポリベンゾオキサゾール樹脂前駆体の製造方法およびポリベンゾオキサゾール樹脂の製造方法
WO2005099656A2 (en) 2004-04-06 2005-10-27 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
AU2005236055B2 (en) 2004-04-20 2011-10-06 Transtech Pharma, Llc Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators
DE102004021716A1 (de) 2004-04-30 2005-12-01 Grünenthal GmbH Substituierte Imidazo[1,2-a]pyridin-Verbindungen und Arzneimittel enthaltend substituierte Imidazo[1,2-a]pyridin-Verbindungen
EP1745036A2 (en) 2004-05-03 2007-01-24 Boehringer Ingelheim Pharmaceuticals Inc. Cytokine inhibitors
PE20060748A1 (es) 2004-09-21 2006-10-01 Smithkline Beecham Corp Derivados de indolcarboxamida como inhibidores de quinasa ikk2
WO2006034337A2 (en) 2004-09-23 2006-03-30 Wyeth Carbazole and cyclopentaindole derivatives to treat infection with hepatitis c virus
EP1812439B2 (en) 2004-10-15 2017-12-06 Takeda Pharmaceutical Company Limited Kinase inhibitors
AU2005304473A1 (en) 2004-11-10 2006-05-18 Cgi Pharmaceuticals, Inc. Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity
DE102004054665A1 (de) 2004-11-12 2006-05-18 Bayer Cropscience Gmbh Substituierte bi- und tricyclische Pyrazol-Derivate Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren
WO2006094235A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Fused heterocyclic compounds and their use as sirtuin modulators
MX2007011041A (es) 2005-03-10 2008-02-22 Cgi Pharmaceuticals Inc Ciertas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas.
JP2006290883A (ja) 2005-03-17 2006-10-26 Nippon Nohyaku Co Ltd 置換ヘテロ環カルボン酸アニリド誘導体、その中間体及び農園芸用薬剤並びにその使用方法
DK2439273T3 (da) 2005-05-09 2019-06-03 Ono Pharmaceutical Co Humane monoklonale antistoffer til programmeret død-1(pd-1) og fremgangsmåder til behandling af cancer ved anvendelse af anti-pd-1- antistoffer alene eller i kombination med andre immunterapeutika
CA2609299A1 (en) 2005-05-20 2006-11-23 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
PT1907424E (pt) 2005-07-01 2015-10-09 Squibb & Sons Llc Anticorpos monoclonais humanos para o ligando 1 de morte programada (pd-l1)
US20080220968A1 (en) 2005-07-05 2008-09-11 Ge Healthcare Bio-Sciences Ab [1, 2, 4] Triazolo [1, 5-A] Pyrimidine Derivatives as Chromatographic Adsorbent for the Selective Adsorption of Igg
WO2007034282A2 (en) 2005-09-19 2007-03-29 Pfizer Products Inc. Diaryl-imidazole compounds condensed with a heterocycle as c3a receptor antagonists
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
US7723336B2 (en) 2005-09-22 2010-05-25 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
CA2628074C (en) 2005-10-25 2014-01-14 Shionogi & Co., Ltd. Aminodihydrothiazine derivative
JP5249772B2 (ja) 2005-11-22 2013-07-31 メルク・シャープ・アンド・ドーム・コーポレーション キナーゼの阻害剤として有用な三環式化合物
WO2007067711A2 (en) 2005-12-08 2007-06-14 Amphora Discovery Corporation Certain chemical entities, compositions, and methods for modulating trpv1
WO2007069565A1 (ja) 2005-12-12 2007-06-21 Ono Pharmaceutical Co., Ltd. 二環式複素環化合物
US20090281075A1 (en) 2006-02-17 2009-11-12 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
WO2007096764A2 (en) 2006-02-27 2007-08-30 Glenmark Pharmaceuticals S.A. Bicyclic heteroaryl derivatives as cannabinoid receptor modulators
WO2007102531A1 (ja) 2006-03-08 2007-09-13 Takeda Pharmaceutical Company Limited 併用薬
MX2008012617A (es) 2006-03-31 2008-10-10 Novartis Ag Compuestos organicos.
WO2008118122A2 (en) 2006-05-08 2008-10-02 Molecular Neuroimaging, Llc Compounds and amyloid probes thereof for therapeutic and imaging uses
CA2691214A1 (en) 2006-06-09 2007-12-21 Kemia, Inc. Therapy using cytokine inhibitors
US20080280891A1 (en) 2006-06-27 2008-11-13 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
AU2007275221A1 (en) 2006-07-20 2008-01-24 Allen J. Borchardt Benzothiophene inhibitors of RHO kinase
DE102006035018B4 (de) 2006-07-28 2009-07-23 Novaled Ag Oxazol-Triplett-Emitter für OLED-Anwendungen
WO2008021745A2 (en) 2006-08-16 2008-02-21 Itherx Pharmaceuticals, Inc. Hepatitis c virus entry inhibitors
TWI389895B (zh) 2006-08-21 2013-03-21 Infinity Discovery Inc 抑制ｂｃｌ蛋白質與結合夥伴間之交互作用的化合物及方法
WO2008027812A2 (en) 2006-08-28 2008-03-06 Forest Laboratories Holdings Limited Imidazopyridine and imidazopyrimidine derivatives
CA2663178C (en) 2006-09-11 2016-01-12 Matrix Laboratories Ltd. Dibenzofuran derivatives as inhibitors of pde-4 and pde-10
US7838523B2 (en) 2006-09-11 2010-11-23 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
AR063706A1 (es) 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
PE20081370A1 (es) 2006-09-11 2008-11-28 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas
WO2008033858A2 (en) 2006-09-11 2008-03-20 Cgi Pharmaceuticals, Inc. Kinase inhibitors, and methods of using and identifying kinase inhibitors
FR2906250B1 (fr) 2006-09-22 2008-10-31 Sanofi Aventis Sa Derives de 2-aryl-6phenyl-imidazo(1,2-a) pyridines, leur preparation et leur application en therapeutique
JP2010507674A (ja) 2006-10-27 2010-03-11 ワイス エルエルシー マトリクスメタロプロテアーゼ阻害剤としての三環式化合物
SI2089364T1 (sl) 2006-11-08 2013-10-30 Bristol-Myers Squibb Company Spojine piridinona
GB0623209D0 (en) 2006-11-21 2007-01-03 F2G Ltd Antifungal agents
WO2008064318A2 (en) 2006-11-22 2008-05-29 University Of Medicine And Dentistry Of New Jersey Peripheral opioid receptor active compounds
WO2008064317A1 (en) 2006-11-22 2008-05-29 University Of Medicine And Dentistry Of New Jersey Lipophilic opioid receptor active compounds
WO2008071944A1 (en) 2006-12-14 2008-06-19 Boehringer Ingelheim International Gmbh Benzoxazoles useful in the treatment of inflammation
CA2673038C (en) 2006-12-22 2015-12-15 Incyte Corporation Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
EP1964841A1 (en) 2007-02-28 2008-09-03 sanofi-aventis Imidazo[1,2-a]azine and their use as pharmaceuticals
EP2137158A4 (en) 2007-02-28 2012-04-18 Methylgene Inc LOW-MOLECULAR INHIBITORS OF PROTEINARGININE METHYLTRANSFERASES (PRMTS)
EP1964840A1 (en) 2007-02-28 2008-09-03 sanofi-aventis Imidazo[1,2-a]pyridines and their use as pharmaceuticals
JP2008218327A (ja) 2007-03-07 2008-09-18 Hitachi Ltd 電解質、電解質膜、それを用いた膜電極接合体、燃料電池電源及び燃料電池電源システム
JP2010120852A (ja) * 2007-03-09 2010-06-03 Daiichi Sankyo Co Ltd 新規なジアミド誘導体
CA2680761A1 (en) 2007-03-22 2008-09-25 Astrazeneca Ab Quinoline derivatives for the treatment of inflammatory diseases
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
JP5383484B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 環式基で置換されたアミノジヒドロチアジン誘導体
WO2008134553A1 (en) 2007-04-26 2008-11-06 Xenon Pharmaceuticals Inc. Methods of using bicyclic compounds in treating sodium channel-mediated diseases
ES2395583T3 (es) 2007-05-10 2013-02-13 Ge Healthcare Limited IMIDAZOL (1,2-A)PIRIDINAS y compuestos relacionados con actividad frente a los receptores cannabinoides CB2
BR122017025062B8 (pt) 2007-06-18 2021-07-27 Merck Sharp & Dohme anticorpo monoclonal ou fragmento de anticorpo para o receptor de morte programada humano pd-1, polinucleotídeo e composição compreendendo o referido anticorpo ou fragmento
WO2009027733A1 (en) 2007-08-24 2009-03-05 Astrazeneca Ab (2-pyridin-3-ylimidazo[1,2-b]pyridazin-6-yl) urea derivatives as antibacterial agents
CL2008002793A1 (es) * 2007-09-20 2009-09-04 Cgi Pharmaceuticals Inc Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras
AU2008302746B2 (en) 2007-09-20 2014-07-03 Amgen Inc. 1-(4-(benzylbenzamid0) -benzyl) azetidine-3-carboxylic acid derivatives and related compounds as SlP receptor modulators for the treatment of immune disorders
DE102007048716A1 (de) 2007-10-11 2009-04-23 Merck Patent Gmbh Imidazo[1,2-a]pyrimidinderivate
TW200932219A (en) 2007-10-24 2009-08-01 Astellas Pharma Inc Oxadiazolidinedione compound
JP2011500778A (ja) 2007-10-25 2011-01-06 アストラゼネカ・アクチエボラーグ ピリジン及びピラジン誘導体−０８３
US7868001B2 (en) 2007-11-02 2011-01-11 Hutchison Medipharma Enterprises Limited Cytokine inhibitors
WO2009062059A2 (en) 2007-11-08 2009-05-14 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
AU2008335761B2 (en) 2007-12-13 2014-04-24 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
RU2364597C1 (ru) 2007-12-14 2009-08-20 Андрей Александрович Иващенко ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ Hh-СИГНАЛЬНОГО КАСКАДА, ЛЕКАРСТВЕННЫЕ КОМПОЗИЦИИ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ, СВЯЗАННЫХ С АББЕРАНТНОЙ АКТИВНОСТЬЮ Hh СИГНАЛЬНОЙ СИСТЕМЫ
JP2011506514A (ja) 2007-12-19 2011-03-03 シンジェンタ パーティシペーションズ アクチェンゲゼルシャフト 殺虫性化合物
WO2009086303A2 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
JP2011506487A (ja) 2007-12-21 2011-03-03 ザ・ユニバーシティ・オブ・シドニー トランスロケータータンパク質リガンド
PL2233474T3 (pl) 2008-01-18 2015-12-31 Eisai R&D Man Co Ltd Skondensowana pochodna aminodihydrotiazyny
JP5381718B2 (ja) 2008-01-31 2014-01-08 コニカミノルタ株式会社 ハロ多環芳香族化合物及びその製造方法
MX2010009416A (es) 2008-02-26 2010-09-24 Novartis Ag Compuestos heterociclicos como inhibidores de cxcr2.
EP2095818A1 (en) 2008-02-29 2009-09-02 AEterna Zentaris GmbH Use of LHRH antagonists at non-castrating doses
EP2262837A4 (en) 2008-03-12 2011-04-06 Merck Sharp & Dohme PD-1 BINDING PROTEINS
FR2928921B1 (fr) 2008-03-21 2010-04-23 Sanofi Aventis Derives polysubstitues de 2-aryl-6-phenyl-imidazo°1,2-a!pyridines, leur preparation et leur application en therapeutique
FR2928924B1 (fr) 2008-03-21 2010-04-23 Sanofi Aventis Derives polysubstitues de 6-heteroaryle-imidazo°1,2-a! pyridines, leur preparation et leur application en therapeutique
FR2928922B1 (fr) 2008-03-21 2010-04-23 Sanofi Aventis Derives de 2-aryl-6-phenyl-imidazo°1,2-a!pyridines polysubstitues, leur preparation et leur application en therapeutique
US8461163B2 (en) 2008-03-31 2013-06-11 Takeda Pharmaceutical Company Limited Substituted N-(pyrazolo[1,5-a]pyrimidin-5-yl)amides as inhibitors of apoptosis signal-regulating kinase 1
KR101034351B1 (ko) 2008-05-14 2011-05-16 한국화학연구원 신규 벤즈옥사졸로 치환된 피리딘 유도체 또는 이의약학적으로 허용가능한 염, 이의 제조방법 및 이를유효성분으로 함유하는 이상세포 성장 질환의 예방 및치료용 약학적 조성물
CA2724842A1 (en) 2008-05-19 2009-11-26 Sunovion Pharmaceuticals Inc. Imidazo[1,2-a]pyridine compounds
WO2009146358A1 (en) 2008-05-29 2009-12-03 Sirtris Pharmaceuticals, Inc. Imidazopyridine and related analogs as sirtuin modulators
US8163743B2 (en) 2008-06-05 2012-04-24 GlaxoGroupLimited 4-carboxamide indazole derivatives useful as inhibitors of PI3-kinases
US8476430B2 (en) 2008-07-24 2013-07-02 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
US9540322B2 (en) 2008-08-18 2017-01-10 Yale University MIF modulators
US9643922B2 (en) 2008-08-18 2017-05-09 Yale University MIF modulators
JP2011231017A (ja) 2008-09-09 2011-11-17 Nissan Chem Ind Ltd 光学活性エポキシ化合物及び光学活性スルホキシド化合物の製造方法、並びに該方法に用いる配位子、錯体及び該錯体の製造方法
US8552154B2 (en) 2008-09-26 2013-10-08 Emory University Anti-PD-L1 antibodies and uses therefor
US8598174B2 (en) 2008-11-12 2013-12-03 Genetech, Inc. Pyridazinones, method of making, and method of use thereof
EP2376490B1 (en) 2008-12-04 2013-01-23 Proximagen Limited Imidazopyridine compounds
EP3255060A1 (en) 2008-12-09 2017-12-13 F. Hoffmann-La Roche AG Anti-pd-l1 antibodies and their use to enhance t-cell function
ES2539620T3 (es) 2008-12-19 2015-07-02 Cephalon, Inc. Pirrolotriazina como inhibidor de ALK y de JAK2
EP2370407B1 (en) 2008-12-19 2014-06-18 Bristol-Myers Squibb Company Carbazole and carboline kinase inhibitors
US8084620B2 (en) 2008-12-19 2011-12-27 Bristol-Myers Squibb Company Carbazole carboxamide compounds useful as kinase inhibitors
JP5624275B2 (ja) 2008-12-22 2014-11-12 ユー・ディー・シー アイルランド リミテッド 有機電界発光素子
SG172352A1 (en) 2008-12-23 2011-07-28 Abbott Lab Anti-viral compounds
JP5578490B2 (ja) 2008-12-26 2014-08-27 味の素株式会社 ピラゾロピリミジン化合物
JP5844159B2 (ja) 2009-02-09 2016-01-13 ユニヴェルシテ デクス−マルセイユＵｎｉｖｅｒｓｉｔｅ Ｄ’Ａｉｘ−Ｍａｒｓｅｉｌｌｅ Ｐｄ−１抗体およびｐｄ−ｌ１抗体ならびにその使用
JP2010202530A (ja) 2009-02-27 2010-09-16 Tokyo Institute Of Technology 含ヘテロ芳香族化合物および光学材料
KR20100101055A (ko) 2009-03-07 2010-09-16 주식회사 메디젠텍 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 ｇｓｋ３ 이동 관련 질환의 치료 또는 예방용 약학적 조성물
MY159575A (en) 2009-04-02 2017-01-13 Merck Serono Sa Dihydroorotate dehydrogenase inhibitors
BRPI1014572B8 (pt) 2009-04-16 2022-07-19 Fundacion Centro Nac De Investigaciones Oncologicas Carlos Iii Imidazopirazinas para uso como inibidores de cinase
US8338441B2 (en) 2009-05-15 2012-12-25 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
US8993604B2 (en) 2009-06-30 2015-03-31 Siga Technologies, Inc. Treatment and prevention of dengue virus infections
WO2011002635A1 (en) 2009-06-30 2011-01-06 Siga Technologies, Inc. Treatment and prevention of dengue virus infections
TWI598347B (zh) 2009-07-13 2017-09-11 基利科學股份有限公司 調節細胞凋亡信號之激酶的抑制劑
JP2011057661A (ja) 2009-08-14 2011-03-24 Bayer Cropscience Ag 殺虫性カルボキサミド類
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US9095596B2 (en) 2009-10-15 2015-08-04 Southern Research Institute Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such
KR101972992B1 (ko) 2009-10-16 2019-04-29 멜린타 서브시디어리 코프. 항미생물성 화합물 및 이의 제조 방법 및 사용 방법
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
WO2011066342A2 (en) 2009-11-24 2011-06-03 Amplimmune, Inc. Simultaneous inhibition of pd-l1/pd-l2
WO2011078221A1 (ja) 2009-12-24 2011-06-30 味の素株式会社 イミダゾピリダジン化合物
WO2011082400A2 (en) * 2010-01-04 2011-07-07 President And Fellows Of Harvard College Modulators of immunoinhibitory receptor pd-1, and methods of use thereof
US20130085133A1 (en) 2010-02-08 2013-04-04 Sourthern Research Institute Office of Commercialization and Intellectual Prop. Anti-viral treatment and assay to screenfor anti-viral agent
TW201136919A (en) 2010-03-02 2011-11-01 Merck Sharp & Amp Dohme Corp Inhibitors of hepatitis C virus NS5B polymerase
EP2542076B1 (en) 2010-03-04 2021-01-13 Merck Sharp & Dohme Corp. Inhibitors of catechol o-methyl transferase and their use in the treatment of psychotic disorders
CA2793086C (en) 2010-03-18 2018-08-21 Institut Pasteur Korea Substituted imidazo[1,2-a]pyridine compounds and their use in the treatment of bacterial infections
US8410117B2 (en) 2010-03-26 2013-04-02 Hoffmann-La Roche Inc. Imidazopyrimidine derivatives
WO2011159857A1 (en) 2010-06-16 2011-12-22 Bristol-Myers Squibb Company Carboline carboxamide compounds useful as kinase inhibitors
WO2011159877A2 (en) 2010-06-18 2011-12-22 The Brigham And Women's Hospital, Inc. Bi-specific antibodies against tim-3 and pd-1 for immunotherapy in chronic immune conditions
CN102295642B (zh) 2010-06-25 2016-04-06 中国人民解放军军事医学科学院毒物药物研究所 2-芳基咪唑并[1,2-a]吡啶-3-乙酰胺衍生物、其制备方法及用途
US8907053B2 (en) 2010-06-25 2014-12-09 Aurigene Discovery Technologies Limited Immunosuppression modulating compounds
EP2402345A1 (en) 2010-06-29 2012-01-04 Basf Se Pyrazole fused bicyclic compounds
CN101891895B (zh) 2010-07-28 2011-11-30 南京航空航天大学 基于桥联双水杨醛结构的苯并噻唑类金属配位聚合物及其制法及应用
WO2012016133A2 (en) 2010-07-29 2012-02-02 President And Fellows Of Harvard College Ros1 kinase inhibitors for the treatment of glioblastoma and other p53-deficient cancers
US8633200B2 (en) 2010-09-08 2014-01-21 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
CN101993415B (zh) 2010-09-15 2013-08-14 北京韩美药品有限公司 作为Hedgehog通路抑制剂的化合物以及包含该化合物的药物组合物及其应用
US8921381B2 (en) 2010-10-04 2014-12-30 Baruch S. Blumberg Institute Inhibitors of secretion of hepatitis B virus antigens
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
CN103282034A (zh) 2010-11-18 2013-09-04 利亘制药公司 造血生长因子模拟物的用途
CN103261188A (zh) 2010-12-17 2013-08-21 先正达参股股份有限公司 杀虫化合物
TWI617559B (zh) 2010-12-22 2018-03-11 江蘇恆瑞醫藥股份有限公司 ２－芳基咪唑并［１，２－ｂ］嗒．２－苯基咪唑并［１，２－ａ］吡啶，和２－苯基咪唑并［１，２－ａ］吡衍生物
PT2661433T (pt) 2011-01-04 2017-10-24 Novartis Ag Compostos de indole ou seus análogos úteis para o tratamento da degeneração macular relacionada com a idade (amd)
WO2012100342A1 (en) 2011-01-27 2012-08-02 Université de Montréal Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators
US8921368B2 (en) 2011-03-17 2014-12-30 Bristol-Myers Squibb Company Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases
US9464065B2 (en) 2011-03-24 2016-10-11 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
BR112013026341A2 (pt) 2011-04-13 2019-09-24 Merck Sharp & Dohe Corp composto, composição farmacêutica, e, método para tratar, prevenir e/ou atrasar o início de uma doença ou patologia
CN102796103A (zh) 2011-05-23 2012-11-28 南京英派药业有限公司 6-（芳基甲酰）咪唑并[1,2-a]嘧啶和6-（芳基甲酰）[1,2,4]三唑并[4,3-a]嘧啶作为Hedgehog抑制剂及其应用
JP6007417B2 (ja) 2011-05-31 2016-10-12 レセプトス エルエルシー 新規ｇｌｐ−１受容体安定剤および調節剤
GB201109763D0 (en) 2011-06-10 2011-07-27 Ucl Business Plc Compounds
WO2012175991A1 (en) 2011-06-24 2012-12-27 Pharminox Limited Fused pentacyclic anti - proliferative compounds
ES2548414T3 (es) 2011-07-08 2015-10-16 Novartis Ag Novedosos derivados de pirrolo pirimidina
EP2548877A1 (en) * 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
WO2013033901A1 (en) 2011-09-08 2013-03-14 Merck Sharp & Dohme Corp. Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases
WO2013040528A1 (en) 2011-09-16 2013-03-21 Microbiotix, Inc. Antimicrobial compounds
US9351973B2 (en) 2011-09-22 2016-05-31 Merck Sharp & Dohme Corp. Pyrazolopyridyl compounds as aldosterone synthase inhibitors
JP6040677B2 (ja) 2011-09-29 2016-12-07 東洋インキＳｃホールディングス株式会社 太陽電池封止材用樹脂組成物
US9284284B2 (en) 2011-10-13 2016-03-15 Novartis Ag Oxazine derivatives and their use in the treatment of disease
RU2014120180A (ru) 2011-10-20 2015-11-27 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Замещенные бициклические аза-гетероциклы и аналоги в качестве модуляторов сиртуина
CA2852615A1 (en) 2011-10-21 2013-04-25 Torrent Pharmaceuticals Limited Novel substituted imidazopyrimidines as gpbar1 receptor modulators
WO2013120040A1 (en) 2012-02-10 2013-08-15 Children's Medical Center Corporation Targeted pathway inhibition to improve muscle structure, function and activity in muscular dystrophy
US9034882B2 (en) 2012-03-05 2015-05-19 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
KR20140131955A (ko) 2012-03-09 2014-11-14 카나 바이오사이언스 인코포레이션 신규 트리아진 유도체
WO2013157021A1 (en) * 2012-04-20 2013-10-24 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
UY34750A (es) 2012-04-20 2013-11-29 Gilead Sciences Inc ?compuestos para el tratamiento del hiv, composiciones,métodos de preparación, intermediarios y métodos terapéuticos?.
WO2013163404A1 (en) 2012-04-27 2013-10-31 The Uab Research Foundation TREATING VIRAL INFECTIONS HAVING VIRAL RNAs TRANSLATED BY A NON-IRES MEDIATED MECHANISM
JP6168055B2 (ja) 2012-06-18 2017-07-26 住友化学株式会社 縮合複素環化合物
WO2014007228A1 (ja) 2012-07-03 2014-01-09 小野薬品工業株式会社 ソマトスタチン受容体作動活性を有する化合物およびその医薬用途
CN104619709B (zh) 2012-07-13 2016-11-09 Ucb生物制药私人有限公司 作为tnf活性调节剂的咪唑并吡啶衍生物
GB201212513D0 (en) 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
JP2015178457A (ja) 2012-07-25 2015-10-08 杏林製薬株式会社 ピラゾロピリジン誘導体、またはその薬理学的に許容される塩
EP2892899B1 (en) 2012-09-06 2018-03-21 Bristol-Myers Squibb Company Imidazopyridazine jak3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases
AU2013322736A1 (en) 2012-09-26 2015-02-26 F. Hoffmann-La Roche Ag Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
WO2014061693A1 (ja) 2012-10-17 2014-04-24 塩野義製薬株式会社 新規非芳香族炭素環又は非芳香族複素環誘導体
US9657024B2 (en) 2012-11-21 2017-05-23 Stategics, Inc. Substituted triazolo-pyrimidine compounds for modulating cell proliferation, differentiation and survival
JP6037804B2 (ja) 2012-12-03 2016-12-07 富士フイルム株式会社 ガス分離膜
PE20191245A1 (es) 2013-01-15 2019-09-18 Incyte Holdings Corp Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim
CN104968660A (zh) 2013-01-22 2015-10-07 霍夫曼-拉罗奇有限公司 作为bace1抑制剂的氟-[1,3]噁嗪类化合物
CN103933036B (zh) 2013-01-23 2017-10-13 中国人民解放军军事医学科学院毒物药物研究所 2‑芳基咪唑并[1,2‑α]吡啶‑3‑乙酰胺衍生物在制备防治PTSD的药物中的用途
WO2014121085A1 (en) 2013-01-31 2014-08-07 Thomas Jefferson University Pd-l1 and pd-l2-based fusion proteins and uses thereof
NZ708593A (en) 2013-02-27 2018-01-26 Mochida Pharm Co Ltd Novel pyrazole derivative
MX374512B (es) 2013-03-08 2025-03-06 Amgen Inc Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y métodos de uso.
CN104045552B (zh) 2013-03-13 2019-06-11 江苏先声药业有限公司 作为神经保护剂的药用化合物
CN105283552A (zh) 2013-03-13 2016-01-27 澳大利亚核科学和技术组织 具有非功能性tspo基因的转基因非人类生物体
WO2014152536A2 (en) 2013-03-14 2014-09-25 Celtaxsys, Inc. Inhibitors of leukotriene a4 hydrolase
EP3495357B1 (en) 2013-03-14 2021-05-05 The Trustees of Columbia University in the City of New York 4-phenylpiperidines, their preparation and use
JP2016512558A (ja) 2013-03-14 2016-04-28 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ヒト免疫不全ウイルス複製の阻害剤
SG11201507395PA (en) 2013-03-14 2015-10-29 Curadev Pharma Private Ltd Inhibitors of the kynurenine pathway
US9308236B2 (en) 2013-03-15 2016-04-12 Bristol-Myers Squibb Company Macrocyclic inhibitors of the PD-1/PD-L1 and CD80(B7-1)/PD-L1 protein/protein interactions
WO2014181287A1 (en) 2013-05-09 2014-11-13 Piramal Enterprises Limited Heterocyclyl compounds and uses thereof
WO2014210255A1 (en) 2013-06-26 2014-12-31 Abbvie Inc. Primary carboxamides as btk inhibitors
CA2917262A1 (en) 2013-07-02 2015-01-08 Syngenta Participations Ag Pesticidally active bi- or tricyclic heterocycles with sulfur containing substituents
AU2014291142B2 (en) 2013-07-17 2018-10-11 Otsuka Pharmaceutical Co., Ltd. Cyanotriazole compounds
US9975896B2 (en) 2013-07-25 2018-05-22 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
EP2835375A1 (en) 2013-08-09 2015-02-11 Fundació Institut Català d'Investigació Química Bis-salphen compounds and carbonaceous material composites comprising them
KR101715090B1 (ko) 2013-08-28 2017-03-13 한국화학연구원 신규한 화합물 또는 이의 약학적으로 허용가능한 염, 및 이를 유효성분으로 함유하는 인플루엔자 바이러스 감염으로 인한 질환의 예방 또는 치료용 약학적 조성물
CN105705489B (zh) * 2013-09-04 2019-04-26 百时美施贵宝公司 用作免疫调节剂的化合物
HUE038169T2 (hu) 2013-09-06 2018-09-28 Aurigene Discovery Tech Ltd 1,2,4-Oxadiazol származékok mint immunomodulátorok
EA029661B1 (ru) 2013-09-06 2018-04-30 Ауриген Дискавери Текнолоджиз Лимитед Производные 1,3,4-оксадиазола и 1,3,4-тиадиазола в качестве иммуномодуляторов
WO2015036927A1 (en) 2013-09-10 2015-03-19 Aurigene Discovery Technologies Limited Immunomodulating peptidomimetic derivatives
JP6336870B2 (ja) 2013-09-30 2018-06-06 日本ポリプロ株式会社 ビフェノール化合物及びそれを用いるオレフィン重合用触媒並びにオレフィン重合体の製造方法
FR3012140B1 (fr) 2013-10-18 2016-08-26 Arkema France Unite et procede pour la purification de methacrylate de methyle brut
GB201321743D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
GB201321746D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
GB201321733D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
GB201321736D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
WO2015095337A2 (en) 2013-12-18 2015-06-25 The Rockefeller University PYRAZOLO[1,5-a]PYRIMIDINECARBOXAMIDE DERIVATIVES FOR TREATING COGNITIVE IMPAIRMENT
MX2016008653A (es) 2014-01-03 2016-09-26 Bayer Animal Health Gmbh Nuevas pirazolil-heteroarilamidas como agentes plaguicidas.
EP3105251A4 (en) 2014-02-10 2017-11-15 Merck Sharp & Dohme Corp. Antibodies that bind to human tau and assay for quantifying human tau using the antibodies
US9732103B2 (en) 2014-02-25 2017-08-15 Achillion Pharmaceuticals, Inc. Carbamate, ester, and ketone compounds for treatment of complement mediated disorders
US9394365B1 (en) 2014-03-12 2016-07-19 Yeda Research And Development Co., Ltd Reducing systemic regulatory T cell levels or activity for treatment of alzheimer's disease
JP6490464B2 (ja) 2014-03-26 2019-03-27 三井化学株式会社 遷移金属化合物、オレフィン重合用触媒およびオレフィン系重合体の製造方法
US10167257B2 (en) 2014-04-04 2019-01-01 Iomet Pharma Ltd. Indole derivatives for use in medicine
US9850225B2 (en) * 2014-04-14 2017-12-26 Bristol-Myers Squibb Company Compounds useful as immunomodulators
CN106661001A (zh) 2014-05-14 2017-05-10 哈佛学院院长等 有机发光二极管材料
WO2015197028A1 (en) 2014-06-28 2015-12-30 Sunshine Lake Pharma Co., Ltd. Compounds as hepatitis c virus (hcv) inhibitors and uses thereof in medicine
CN104211726B (zh) 2014-08-11 2017-06-16 中南民族大学 非茂类三齿双核钛配合物、制备方法及用途
WO2016044604A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
JP6777638B2 (ja) 2014-09-19 2020-10-28 マッカイ メディカル ファンデーション ザ プレスビュテロス チャーチ イン タイワン マッカイ メモリアル ホスピタル ベンゾ複素環化合物および薬剤
US10253023B2 (en) 2014-10-06 2019-04-09 Merck Patent Gmbh Heteroaryl compounds as BTK inhibitors and uses thereof
EP3230279A1 (en) 2014-12-10 2017-10-18 Massachusetts Institute of Technology Fused 1,3-azole derivatives useful for the treatment of proliferative diseases
JP6853619B2 (ja) 2015-01-16 2021-03-31 大塚製薬株式会社 シアノトリアゾール化合物の医薬用途
DE112016000383B4 (de) 2015-01-20 2026-05-07 Samsung Display Co., Ltd. Organische Moleküle, deren Verwendung in optoelektronischen Bauelementen, optoelektronisches Bauelement und Verfahren zu dessen Herstellung
WO2016118404A1 (en) 2015-01-20 2016-07-28 Merck Sharp & Dohme Corp. Iminothiadiazine dioxides bearing an amine-linked substituent as bace inhibitors, compositions, and their use
WO2016156282A1 (en) 2015-04-02 2016-10-06 Bayer Cropscience Aktiengesellschaft Novel triazole compounds for controlling phytopathogenic harmful fungi
WO2017035405A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amino compounds for treatment of immune and inflammatory disorders
US10745382B2 (en) 2015-10-15 2020-08-18 Bristol-Myers Squibb Company Compounds useful as immunomodulators
WO2017070089A1 (en) 2015-10-19 2017-04-27 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2017070320A1 (en) 2015-10-21 2017-04-27 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Phenyl indole allosteric inhibitors of p97 atpase
US9603950B1 (en) 2015-10-25 2017-03-28 Institute Of Nuclear Energy Research Compounds of imaging agent with HDAC inhibitor for treatment of Alzheimer syndrome and method of synthesis thereof
KR101717601B1 (ko) 2015-11-10 2017-03-20 한국화학연구원 신규한 화합물 또는 이의 약학적으로 허용가능한 염, 및 이를 유효성분으로 함유하는 인플루엔자 바이러스 감염으로 인한 질환의 예방 또는 치료용 약학적 조성물
SG10202004618TA (en) 2015-11-19 2020-06-29 Incyte Corp Heterocyclic compounds as immunomodulators
MA44075A (fr) 2015-12-17 2021-05-19 Incyte Corp Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1
AU2016379372A1 (en) 2015-12-22 2018-08-02 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2017107052A1 (en) 2015-12-22 2017-06-29 Merck Sharp & Dohme Corp. Soluble guanylate cyclase stimulators
HRP20210698T1 (hr) 2015-12-22 2021-09-17 Immatics Biotechnologies Gmbh Peptidi i kombinacija peptida za uporabu u imunoterapiji protiv karcinoma dojke i drugih karcinoma
US10750742B2 (en) 2015-12-22 2020-08-25 Syngenta Participations Ag Pesticidally active pyrazole derivatives
EA036205B1 (ru) 2015-12-22 2020-10-14 Синтон Б.В. Фармацевтическая композиция, содержащая аморфный леналидомид и антиоксидант
KR101653560B1 (ko) 2016-02-02 2016-09-12 한국화학연구원 신규한 화합물 또는 이의 약학적으로 허용가능한 염, 및 이를 유효성분으로 함유하는 인플루엔자 바이러스 감염으로 인한 질환의 예방 또는 치료용 약학적 조성물
TWI833686B (zh) 2016-04-22 2024-03-01 美商英塞特公司 Lsd1 抑制劑之調配物
AR108396A1 (es) 2016-05-06 2018-08-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
WO2017205464A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
KR102518451B1 (ko) 2016-06-20 2023-04-04 엘랑코 유에스 인코포레이티드 Peg화된 돼지 인터페론 및 그의 사용 방법
HUE060256T2 (hu) 2016-06-20 2023-02-28 Incyte Corp Heterociklusos vegyületek mint immunmodulátorok
ES2975263T3 (es) 2016-06-20 2024-07-04 Novartis Ag Formas cristalinas de un compuesto triazolopirimidínico
ES2870920T3 (es) 2016-06-21 2021-10-28 X4 Pharmaceuticals Inc Inhibidores de CXCR4 y usos de los mismos
EP3484866B1 (en) 2016-07-14 2022-09-07 Incyte Corporation Heterocyclic compounds as immunomodulators
JP2019530732A (ja) 2016-08-03 2019-10-24 アライジング・インターナショナル・インコーポレイテッドＡｒｉｓｉｎｇ Ｉｎｔｅｒｎａｔｉｏｎａｌ， Ｉｎｃ． 免疫モジュレータとして有用な対称または半対称化合物
WO2018044783A1 (en) 2016-08-29 2018-03-08 Incyte Corporation Heterocyclic compounds as immunomodulators
CA3034891A1 (en) 2016-08-30 2018-03-08 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds and methods of treatment
AU2017383236B2 (en) 2016-12-21 2022-02-10 Acerta Pharma B.V. Imidazopyrazine inhibitors of Bruton's tyrosine kinase
TWI795381B (zh) 2016-12-21 2023-03-11 比利時商健生藥品公司 作為ｍａｌｔ１抑制劑之吡唑衍生物
LT3558990T (lt) 2016-12-22 2022-12-27 Incyte Corporation Tetrahidroimidazo[4,5-c]piridino dariniai kaip pd-l1 internalizavimo induktoriai
CN114989205A (zh) 2016-12-22 2022-09-02 卡里塞拉生物科学股份公司 用于抑制精氨酸酶活性的组合物和方法
US20180179202A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018119263A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds derivatives as pd-l1 internalization inducers
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
JP7101678B2 (ja) 2016-12-22 2022-07-15 インサイト・コーポレイション 免疫調節剤としての複素環式化合物
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
US10919852B2 (en) 2017-07-28 2021-02-16 Chemocentryx, Inc. Immunomodulator compounds
US10392405B2 (en) 2017-08-08 2019-08-27 Chemocentryx, Inc. Macrocyclic immunomodulators
EP3669872A4 (en) 2017-08-18 2021-05-05 Shanghai Ennovabio Pharmaceuticals Co., Ltd. FORMYL PYRIDINE DERIVATIVE WITH PD-L1 INHIBITORING EFFECT, MANUFACTURING METHOD FOR IT AND USE THEREOF
SMT202500157T1 (it) 2018-03-30 2025-05-12 Incyte Corp Composti eterociclici come immunomodulatori
JP2021520342A (ja) 2018-04-03 2021-08-19 ベータ ファーマシューティカルズ カンパニー リミテッド 免疫調節物質、組成物及びそれらの方法
TWI712412B (zh) 2018-04-19 2020-12-11 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
HUE061503T2 (hu) 2018-05-11 2023-07-28 Incyte Corp Tetrahidro-imidazo[4,5-C]piridin-származékok mint PD-L1 immunmodulátorok
WO2020086556A1 (en) 2018-10-24 2020-04-30 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
AU2019373702A1 (en) 2018-11-02 2021-06-24 Shanghai Maxinovel Pharmaceuticals Co., Ltd. Diphenyl-like compound, intermediate thereof, preparation method therefor, pharmaceutical composition thereof and uses thereof
US11596692B1 (en) 2018-11-21 2023-03-07 Incyte Corporation PD-L1/STING conjugates and methods of use
MY209609A (en) 2019-01-31 2025-07-24 Betta Pharmaceuticals Co Ltd Immunomodulators, compositions and methods thereof
GB201911210D0 (en) 2019-08-06 2019-09-18 Amlo Biosciences Ltd Clinical management of oropharyngeal squamous cell carcinoma
JP7665593B2 (ja) 2019-08-09 2025-04-21 インサイト・コーポレイション Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩
US20230405105A1 (en) 2019-09-20 2023-12-21 Transgene Sa Combination of a poxvirus encoding hpv polypeptides with an anti-pd-l1 antibody
PE20221038A1 (es) 2019-09-30 2022-06-17 Incyte Corp Compuestos de pirido[3,2-d] pirimidina como inmunomoduladores
CA3160131A1 (en) 2019-11-11 2021-05-20 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
JP2023524530A (ja) 2020-05-04 2023-06-12 ビヨンドスプリング ファーマシューティカルズ，インコーポレイテッド 免疫原性が低い癌の癌細胞死滅を増強するための３剤併用療法
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
CR20230230A (es) 2020-11-06 2023-07-27 Incyte Corp Proceso para hacer un inhibidor de pd-1/pdl1 y sales y formas cristalinas del mismo
US20220193050A1 (en) 2020-12-18 2022-06-23 Incyte Corporation Oral formulation for a pd-l1 inhibitor
WO2023049831A1 (en) 2021-09-24 2023-03-30 Incyte Corporation Treatment of human papillomavirus-associated cancers by pd-l1 inhibitors

Also Published As

Publication number Publication date
MD3472167T2 (ro) 2023-02-28
ES2927984T3 (es) 2022-11-14
RS63673B1 (sr) 2022-11-30
JP2022058400A (ja) 2022-04-12
EP3472167A1 (en) 2019-04-24
EP4137489A1 (en) 2023-02-22
PL3472167T3 (pl) 2022-12-19
JP7394824B2 (ja) 2023-12-08
ZA202405294B (en) 2025-04-30
AU2021250978A1 (en) 2021-11-11
EP3472167B1 (en) 2022-08-03
CA3028685A1 (en) 2017-12-28
CN109890819B (zh) 2022-11-22
BR112018076534A2 (pt) 2019-04-02
TW201800409A (zh) 2018-01-01
KR20190035694A (ko) 2019-04-03
AU2017281285C1 (en) 2022-05-12
US11873309B2 (en) 2024-01-16
KR102685249B1 (ko) 2024-07-17
PE20190731A1 (es) 2019-05-23
CL2018003701A1 (es) 2019-04-05
CO2019000386A2 (es) 2019-04-30
ECSP19003773A (es) 2019-04-30
WO2017222976A1 (en) 2017-12-28
MX2018016273A (es) 2019-07-04
AU2017281285A1 (en) 2019-01-31
UA125391C2 (uk) 2022-03-02
US20210317139A1 (en) 2021-10-14
AU2021250978B2 (en) 2023-11-09
MX2022000789A (es) 2022-02-14
PT3472167T (pt) 2022-11-11
SG11201811414TA (en) 2019-01-30
US20170362253A1 (en) 2017-12-21
HUE060256T2 (hu) 2023-02-28
MY197280A (en) 2023-06-09
US20190040082A1 (en) 2019-02-07
LT3472167T (lt) 2022-11-10
DK3472167T3 (da) 2022-09-05
JP2019523231A (ja) 2019-08-22
SI3472167T1 (sl) 2022-11-30
SG10202012828TA (en) 2021-01-28
PH12018502710A1 (en) 2019-04-15
IL263825A (en) 2019-01-31
IL263825B (en) 2022-08-01
MX389513B (es) 2025-03-20
NZ749960A (en) 2025-06-27
JP7000357B2 (ja) 2022-01-19
AU2017281285B2 (en) 2021-11-04
TWI771305B (zh) 2022-07-21
SMT202200392T1 (it) 2022-11-18
CN109890819A (zh) 2019-06-14
US20190062345A1 (en) 2019-02-28

Similar Documents

Publication Publication Date Title
HRP20221030T1 (hr) Heterociklički spojevi kao imunomodulatori
HRP20221035T1 (hr) Heterociklički spojevi kao imunomodulatori
JP7149276B2 (ja) Ｐｄ－ｌ１内在化誘導物質としてのテトラヒドロイミダゾ［４，５－ｃ］ピリジン誘導体
HRP20210190T1 (hr) Heterociklični spojevi kao imunomodulatori
JP2018529739A5 (hr)
HRP20211920T1 (hr) Inhibitori za pd-1/pd-l1
NZ626942A (en) New indolizine derivatives, method for preparing same and pharmaceutical compositions containing same
CA3215823A1 (en) Heterocyclic derivative inhibitor and preparation method therefor and application thereof
HRP20240368T1 (hr) Heterociklički inhibitori atr kinaze
HRP20171758T1 (hr) Kombinacija dr5 agonista i anti-pd-1 antagonista i načini primjene
SI2793884T1 (en) Inhibitors of notch signalling pathway and use thereof in treatment of cancers
JP2022544946A5 (hr)
ES2392489T3 (es) Dicarbazoles y procedimientos de uso
RU2011129776A (ru) Гетероциклические соединения и способы применения
CN106883193B (zh) 吲哚胺2,3-双加氧酶抑制剂及其制备方法与应用
HRP20192209T1 (hr) Derivati benzofurana, postupci njihove pripreme i njihova uporaba u medicini
HRP20200681T1 (hr) Ciklički eter pirazol-4-il-heterociklil-karboksamidni spojevi i postupci njihove upotrebe
JP2016516821A5 (hr)
JP2009535335A5 (hr)
RU2016130932A (ru) Производные хинолона как ингибиторы рецептора фактора роста фибробластов
RU2018111459A (ru) Гетероциклические соединения и их применение
AR082974A1 (es) Derivados de azabenzotiazol, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos para tratar enfermedades inflamatorias
BRPI0716224A2 (pt) Compostos inibidores de raf e métodos de uso dos mesmos.
JP2011522888A5 (hr)
HRP20190805T1 (hr) Spojevi triazolopirimidina i njihova uporaba